cas 477600-74-1, N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Articles about 477600-74-1Total 38 be found

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Short enantioselective total synthesis of (+)-tofacitinib
An enantioselective total synthesis of Tofacitinib (CP-690,550), a Janus tyrosine kinase (JAK3) specific inhibitor has been achieved from the readily available 4-piperidone. Proline catalysed hydroxylation is the key step for the synthesis of enantiopure 1-benzyl-4-methylpiperidin-3-ol.
Mane, Kishor D.,Kamble, Rohit B.,Suryavanshi, Gurunath
(2021/02/20)

Preparation method of tofacitinib citrate
The invention discloses a preparation method of tofacitinib citrate. The method comprises the following steps: by taking 7-tert-butyloxycarbonyl-4-amino-7H-pyrrolo[2, 3-D]pyrimidine and 1-benzyl-4-methyl-piperidine-3-ketone as initial raw materials, carrying out condensation under a weak acidic condition, then carrying out N methylation, selective reduction, debenzylation and Boc removal, and carrying out ester exchange and citric acid salification at a high temperature to obtain the tofacitinib citrate. The method has the advantages of mild reaction conditions, simple post-treatment mode, reduction of the generation amount of hazardous wastes, environmental protection, cost saving, and facilitation of industrial production.
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(2021/04/21)

Preparation method of tofacitinib hydrolysis impurity
The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of a tofacitinib hydrolysis impurity. The method comprises the following steps: dissolving isopropyl malonate in an organic solvent, adding N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, conducting stirring at room temperature until the reaction is finished, and recrystallizing the reaction solution to obtain the tofacitinib hydrolysis impurity. The synthesis method provided by the invention is simple, the tofacitinib hydrolysis impurity obtainedby the method is recrystallized for separation, the purity is high, the yield is high, and the impurity compound can be used as an impurity reference substance in tofacitinib finished product detection standards.
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Paragraph 0043-0044

(2021/03/31)

Process for the preparation of tofacitinib and intermediates thereof
Provided is a process for the preparation of high purity tofacitinib, which reduces formation of N-methyl impurity. The invention also provides novel intermediates used in the process to prepare tofacitinib. There is provided an improved process for the preparation of tofacitinib (I), comprising the steps of: adding cyanoacetic acid in molar equivalent 0.2-1.2 to compound of formula (II-S), followed by addition of carbodiimide coupling agent of formula (III), optionally reacting tofacitinib base with citric acid.
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(2021/05/07)

Synthesis method of tofacitinib citrate
The invention discloses a tofacitinib citrate synthesis method, belongs to the technical field of tofacitinib citrate preparation, and can effectively inhibit activity of Janus and JAK1 JAK3, block signal transduction of various inflammatory cytokines, and has an expensive catalyst application in the existing synthesis step. The method uses 1 - benzyl -4 - methyl -3 - (methylamino) piperidine hydrochloride as a raw material to prepare the tofacitinib citrate as a raw material, and then the citric acid tofacitinib citrate is obtained through twice refining 4 -7 - and the - 7H - yield and 2 the 3 - D purity of the tofacitinib citrate are improved.
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(2021/12/07)

Synthesis method of tofacitinib key intermediate
The invention relates to a method for preparing high-purity (N-methyl N ((3R, 4R)-4-methylpiperidine-3-yl)-7H-pyrrolo [2, 3-d] pyrimidine-4-amine (tofacitinib key intermediate). According to the method, 4-chloro-7H-pyrrolo [2, 3-d] pyrimidine is taken as an initial raw material, benzyl protection, condensation reaction and dibenzyl protection removal reaction are carried out, and then purification is carried out, so that the product disclosed by the invention is obtained. The purity of the product (N-methyl N ((3R, 4R)-4-methylpiperidine-3-yl)-7H-pyrrolo [2, 3-d] pyrimidine-4-amine is 98% orabove; the total yield of the synthesis method is 80% or above; and the synthesis method is suitable for industrial production.
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(2020/09/09)

PROCESS FOR PREPARATION OF TOFACITINIB AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
The present invention relates to an improved process for preparation of tofacitinib (I) and pharmaceutically acceptable salt thereof. (I)
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(2020/09/27)

PROCESSES FOR PREPARING (3R,4R)-1-BENZYL-N,4-DIMETHYLPIPERIDIN-3-AMINE OR A SALT THEREOF AND PROCESSES FOR PREPARING TOFACITINIB USING THE SAME
The present invention provides a novel process for preparing (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine or a salt thereof, which is an intermediate useful for the preparation of tofacitinib. The present invention also provides a novel intermediate used in the process, i.e., isopropanol solvate of methyl ((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)carbamate dibenzoyl-L-tartrate. The present invention also provides a novel intermediate, having excellent stability, useful for the preparation of tofacitinib, i.e., (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine acetate. In addition, the present invention provides a process for preparing tofacitinib or a pharmaceutically acceptable salt thereof using the process.
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(2020/10/20)

Synthesis method of tofacitinib citrate
The invention relates to the technical field of medicinal chemistry, and discloses a synthesis method of tofacitinib citrate. The method comprises 1) preparing 2,4-dihydroxy pyrrolopyrimidine: adding4-aminouracil and anhydrous sodium acetate into water (in a molar ratio of (1: 3)-(1: 5)), heating to 60-80 DEG C, slowly adding a 2-chloroacetaldehyde aqueous solution having a concentration of 40%,stirring to react for 4-6 hours, cooling to room temperature, filtering, washing a solid with water, and drying under reduced pressure to obtain 2,4-dihydroxy pyrrolopyrimidine. According to the synthesis method of tofacitinib citrate, through two times of impurity removal, the purity of the produced tofacitinib citrate finished product is higher, subsequent purification is not needed, the synthesis time is short, the process is simple, the method is suitable for factory production, the production time of the tofacitinib citrate finished product can be saved, the production efficiency of the tofacitinib citrate finished product is improved, and the tofacitinib citrate is more convenient to use.
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(2020/08/29)

Preparation method of tofacitinib or salt thereof (by machine translation)
The preparation method of the tofacitinib intermediate V compound comprises the following steps: (1) a compound II and a compound III are subjected to a photoreaction reaction to generate an intermediate IV; (2) an intermediate IV and a methylation reagent are subjected to methylation reaction to generate a compound of formula V; wherein R is. 1 And R2 Are each independently an amino protecting group. The preparation method disclosed by the invention does not need to be subjected to isomer resolution purification in the preparation method, avoids using tetrahydroaluminum hydride, is low in synthesis cost, high in yield, simple in reaction condition and post-treatment operation and suitable for industrial production. (by machine translation)
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(2020/06/20)

Preparation method of tofacitinib citrate
The invention relates to the field of medicine synthesis, and particularly discloses a preparation method of tofacitinib citrate. The preparation method comprises the following steps: S1, dissolving acompound SM1, a compound SM2 and an alkaline reagent in a solvent A, and performing a reaction to obtain a first compound; S2, taking and mixing a catalyst, a solvent B and the first compound, introducing hydrogen, and carrying out a catalytic hydrogenation reaction to obtain a second compound; S3, taking and mixing active anhydride, a solvent C and the second compound, and carrying out an acylation reaction to obtain a third compound, wherein R in the active anhydride comprises an alkyl group or an aryl group; and S4, taking and mixing citric acid, a solvent D and the third compound, and carrying out a salt-forming reaction to obtain a compound T that is the tofacitinib citrate. The preparation method has the advantages of easily available initial raw materials, no use of complex or toxic compounds, short synthesis process route, simple and convenient reaction operation of each step, high total yield and high productivity, and is suitable for large-scale industrial production.
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(2020/02/14)

Improved tofacitinib synthesis method and impurity preparation method (by machine translation)
The invention discloses an improved tofacitinib synthesis method and an impurity preparation method. By controlling pH value of the reaction liquid, the impurity type A is decomposed into the compound II, formic acid in the reaction liquid is easily removed, and the reaction yield and the tofacitinib quality are effectively improved. , The invention also provides a synthetic method of the impurity type A, which can be used for synthesizing the impurity type A through the method and detecting and controlling the quality of the tofacitinib. (by machine translation)
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Paragraph 0034-0035; 0038-0039; 0041-0042; 0044-0045; 0047

(2020/12/30)

Preparation method of tofacitinib citrate
The invention discloses a preparation method of tofacitinib citrate. The method comprises the following steps: 1) performing a desalting reaction on a compound represented by a formula II shown in thedescription under basic conditions to obtain an intermediate represented by a formula III shown in the description; 2) in the presence of a basic ionic liquid, performing a reaction on the intermediate represented by the formula III, ethyl cyanoacetate and a base in an inert atmosphere to obtain a reaction liquid containing a tofacitinib base; and 3) adding citric acid monohydrate into the reaction liquid containing the tofacitinib base, and performing a salt formation reaction to obtain the tofacitinib citrate. According to the method provided by the invention, in the preparation process, anappropriate amount of the [Bmim]Im is added, a combination with a specific ratio of triethylamine to pyridine is selected as the base, and the ionic liquid is used as a solvent for the reaction and used as a catalyst to promote rapid progress of the reaction, and improves the yield and purity of the product.
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Paragraph 0042-0045

(2019/07/29)

Method for preparing key intermediate of Tofacitinib
The invention provides a method for preparing a key intermediate (compound I) of Tofacitinib. The key intermediate of Tofacitinib is prepared through subjecting a compound II, which serves as a starting raw material, with a reaction with ammonium formate in the presence of a catalyst. The method for synthesizing the key intermediate of Tofacitinib-compound I, provided by the invention, has the aimof being applicable to industrial production and high-selectivity preparation. Through changing an experimental method, the generating of superhydrogenated impurities is avoided while operations canbe suitable for industrialization, so that the quality of the compound I can be controllable, and the quality of a finished product is better.
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Paragraph 0012-0023

(2019/08/12)

For the prevention and treatment of various autoimmune diseases of the new compound
Disclosed is an isoxazole derivative that inhibits the activity of the Janus kinases (JAKs), the structure thereof as presented in formula I, formula II, formula IX, and formula XI. The substituent groups in the formulas are described in the description. Also disclosed are the pharmaceutical composition of the compound and a related use in medicine preparation.
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(2018/04/20)

JANUS KINASE 1 SELECTIVE INHIBITOR AND PHARMACEUTICAL USE THEREOF
Janus kinase 1 selective inhibitors and pharmaceutical use thereof are provided.
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(2018/06/07)

NOVEL TOFACITINIB ADDITION SALTS AND PROCESS FOR THE PREPARATION THEREOF
The present invention provides several novel Tofacitinib addition salts and their solid state forms, hydrates, solvates and their uses as medicaments thereof.
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(2018/10/19)

Tofacitinib compound preparation method
The invention discloses a tofacitinib compound preparation method. Under alkali and solvent existence condition, 4-methyl piperidine-3-ketamine hydrochloride (II) and benzyl chloride are subjected toa reaction to obtain a compound III, acid catalysis is carried out to obtain a compound V, and steps of asymmetric catalytic hydrogenation, deprotection, and condensation are carried out to obtain a final product tofacitinib (I), the preparation method has the advantages of short technical process, mild reaction condition, high overall yield and purity, and less by-product, and is suitable for industrial preparation.
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(2018/11/27)

Method for preparing Tofacitinib citrate
The invention provides a method for preparing Tofacitinib citrate. The method comprises the steps of hydrochloric acid removal, amidation reaction, salt forming and the like. According to the method,the cost is low, the operation is simple and convenient, and the obtained product is high in purity, so that the method is applicable to industrial large-scale production.
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Paragraph 0087; 0089

(2018/11/22)

Preparation method of tofacitinib citrate
The invention discloses a preparation method of tofacitinib citrate. The preparation method comprises the following steps: stirring an organic solvent, a compound 3, 5 percent wet palladium on carbonand acetic acid until a mixture is suspended; conveying the mixture into a micro-reactor from a channel A; meanwhile, conveying alkylsilane into the micro-reactor from a channel B; controlling the temperature of the micro-reactor to 20 to 30 DEG C and carrying out reaction; carrying out post-treatment to obtain a compound 2; after uniformly mixing an alcohol type solvent, the compound 2, ethyl cyanoacetate and DBU (1,8-Diazabicyclo [5,4,0]undec-7-ene), conveying a mixture into the micro-reactor from the channel A; dissolving citric acid into a mixed solution of water and the alcohol type solvent, conveying a mixture into the micro-reactor from the channel B; controlling the temperature in the micro-reactor to 70 to 80 DEG C and carrying out reaction; cooling and crystallizing to obtain thetofacitinib citrate. The method provided by the invention has the advantages of controllable reaction condition and simplicity in operation; dangers caused by the fact that flammable and explosive gas is used are avoided and the safety is higher; reaction can be finished instantly and the reaction time is greatly shortened; debenzylation reaction and acylation reaction are complete and post-treatment is simple; the preparation method is suitable for industrial large-scale production. A formula is shown in the description.
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(2018/07/30)

Preparation method of tofacitinib key intermediate
The invention discloses a preparation method of a tofacitinib key intermediate with a chemical name as (3R, 4R)-methyl-(4-methyl-piperidine-3-yl)-(7H-pyridine[2,3-d]pyridine-4-yl)amine and the CAS number of 477600-74-1. The preparation method is characterized in that ammonium formate or hydrazine hydrate is used as a hydrogen donator, phenyl and chlorine of the 2-chloro-4-{(methyl)[(3R,4R)-1-benzyl-4-methylpiperidin-3-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine are removed under the catalysis of catalysts such as palladium/carbon hydroxide to generate the intermediate. By adopting the preparation method, no autoclave is used. The preparation method has the advantages of mild reaction conditions, higher safety, high reaction rate, fewer process byproducts, simple operation and higher productivity, can effectively solve the problem that more impurities exist in the preparation process, and facilitates the industrialized production.
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Paragraph 0019; 0021; 0022; 0024

(2018/11/03)

PROCESS FOR THE PREPARATION OF (3R,4R)-4-METHYL-3-(METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL-AMINO)-?-OXO-1-PIPERIDINEPROPANENITRILE AND ITS SALTS
The present invention relates to an improved 7H-pyrrolo[2,3-d]pyrimidin-4-yl-amino)-β-oxo-1-piperidine propanenitrile compound of formula-1 and its pharmaceutically acceptable salts.
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(2016/07/20)

An Efficient Method for Synthesis of Tofacitinib Citrate
An efficient and mild synthetic method was developed for tofacitinib citrate from 3-amino-4-methylpyridine and 4-chloro-7H-pyrrolo[2,3-d]pyrimidine. The related reactions were systematically optimized. Sodium hydride instead of potassium tert-butoxide employed in the methoxycarbonylation reaction of compound 9 made the reaction proceed effectively to present compound 8 in a better yield. The replacement of benzaldehyde with benzyl bromide simplified the protection process of amino group. Red-Al provided a cost-effective method for the reduction of amides. The introduction of tosyl group into compound 10 enhanced the nucleophilic substitution of 10 with compound 4 dramatically. Thus, under the optimized conditions, tofacitinib citrate was obtained in 13.3% yield (based on compound 9) with a purity of 99.9%, much better than the reported yield 8.6%. This cost-effective and environmental friendly process is more suitable for scale-up production.
Zhi, Shuang,Liu, Dengke,Liu, Ying,Liu, Bingni,Wang, Donghua,Chen, Ligong
p. 1259 - 1263
(2016/07/29)

EFFICIENT METHOD FOR THE PREPARATION OF TOFACITINIB CITRATE
Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises: 1. Condensation between intermediates VII and VIII to give intermediate VI 2. Hydrogenation of intermediate VI to give intermediate V 3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99% 4. Release of intermediate IV in a basic medium to give intermediate III 5. N-acylation reaction of intermediate III to give II (tofacitinib) 6. Salification of intermediate II to give tofacitinib monocitrate (I)
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(2016/10/31)

Method for synthesizing citric acid tofacitinib
The invention discloses an efficient and safe method for synthesizing citric acid tofacitinib. N-[(3R,4R)-1-benzyl-4-methylpiperidine-3-base]-N-methyl-7H-pyrrolo[2,3-d]pyrimidine-4-amine is used as the raw material, Pd/C and HCOOH reduction debenzylation is conducted, condensation is conducted under the catalysis of an EDCI or EDCI, HOBT and triethylamine compound system with cyanoacetic acid, and salifying is conducted with citric acid in acetone to obtain citric acid tofacitinib. By the adoption of the synthesis method, potential safety hazards caused by hydrogen and ammonium formate are avoided, debenzylation reaction and amidation are thorough, no side reaction is caused basically, reaction time is shortened greatly, yield is high, aftertreatment is easy, and citric acid tofacitinib can be prepared efficiently and safely.
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Paragraph 0045; 0049; 0050; 0059; 0060; 0061; 0062-0064

(2016/12/26)

Preparation method of JAKs inhibitor drug tofacitinib
The invention discloses a preparation method of JAKs inhibitor drug tofacitinib. The preparation method is characterized by comprising the following steps: (1) taking 2, 4-dichloro-7Hpyrolle[2,3-D]pyrimidine as a raw material to react with halogenated benzyl to prepare a compound II in the existence of alkali; (2) allowing (3R, 4R)-N,4-dimethyl-1-(phenyl-methyl)-3-piperidylamine hydrochloride to react with 7-benzyl-2,4-dichloro-7Hpyrolle[2, 3-D]pyrimidine in the existence of alkali to prepare a compound IV; (3) catalyzing the compound IV obtained in the step (2) to have hydrogenation reaction in the existence of a metal catalyst to obtain a compound V; (4) coupling and joining the compound V obtained in the step (3) with cyanoacetic acid in the existence of a condensation agent to obtain a compound VI; and (5) salifying the compound VI obtained in the step (4) and citric acid to obtain tofacitinib. The method is simple and short in synthetic route, simple in the operation of various reaction processes, capable of recycling the solvents, little in pollution, and suitable for industrialized mass production.
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Paragraph 0018

(2016/10/10)

Synthesis method of JAK inhibitor tofacitinib
The invention relates to a synthesis method of a JAK inhibitor tofacitinib. The method comprises the steps: with N-[(3R,4R)-1-benzyl-4-methylpiperidin-3-yl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine as a raw material, with formic acid, ammonium formate or hydrazine hydrate as a hydrogen donor, carrying out hydrogenation to remove benzyl to obtain N-[(3R,4R)-4-methylpiperidin-3-yl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine, and then carrying out a reaction with cyanoacetic acid to obtain tofacitinib. Compared with an original synthesis method, the method provided by the invention has the advantages of mild conditions, simple and convenient operation, high yield, low cost and the like, and is suitable for industrialized production.
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Paragraph 0035; 0036

(2016/10/31)

Novel synthetic process of tofacitinib citrate
The invention discloses a novel synthetic process of tofacitinib citrate. The novel synthetic process comprises the steps that 1, an initial raw material-1, 10% of palladium on carbon, absolute methanol and ammonium formate are mixed in a reaction container, and reacting is carried out to obtain a midbody-1; 2, the midbody-1 prepared in the step 1 is dissolved into absolute ethyl alcohol, an initial raw material-2 is added, reacting is carried out at the reaction temperature of 20 DEG C to 50 DEG C, reaction liquid is purified to obtain a crude midbody-2 after reacting is finished, and the crude midbody-2 is refined to obtain a refined midbody-2; 3, the refined midbody-2 is subjected to heating reflux and dissolved clarification through absolute ethyl alcohol, a citric acid water solution is dropwise added, and reacting continues to be carried out at the temperature of 50 DEG C to 90 DEG C; then the mixture is slowly cooled to 20 DEG C to 45 DEG C, and stirring and devitrification are carried out; crystals are filtered and washed with ethyl alcohol, drying is carried out under reduced pressure at the temperature of 40 DEG C to 60 DEG C, and white crude tofacitinib citrate is obtained. The chemical synthetic process is more reasonable in route, and the reaction conditions are milder.
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Paragraph 0010; 0048; 0049; 0053; 0054

(2016/10/08)

TOFACITINIB CITRATE
Crystalline particle of tofacitinib citrate, process for the preparation of a crystalline particle of tofacitinib citrate, pharmaceutical composition, substantially pure amorphous form of tofacitinib citrate, process for preparing the substantially pure amorphous form of tofacitinib citrate, and use of the crystalline particle of tofacitinib citrate, and the pharmaceutical composition are provided.
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Page/Page column 12

(2015/04/28)

Novel Hinge-Binding Motifs for Janus Kinase 3 Inhibitors: A Comprehensive Structure-Activity Relationship Study on Tofacitinib Bioisosteres
The Janus kinases (JAKs) are a family of cytosolic tyrosine kinases crucially involved in cytokine signaling. JAKs have been demonstrated to be valid targets in the treatment of inflammatory and myeloproliferative disorders, and two inhibitors, tofacitinib and ruxolitinib, recently received their marketing authorization. Despite this success, selectivity within the JAK family remains a major issue. Both approved compounds share a common 7H-pyrrolo[2,3-d]pyrimidine hinge binding motif, and little is known about modifications tolerated at this heterocyclic core. In the current study, a library of tofacitinib bioisosteres was prepared and tested against JAK3. The compounds possessed the tofacitinib piperidinyl side chain, whereas the hinge binding motif was replaced by a variety of heterocycles mimicking its pharmacophore. In view of the promising expectations obtained from molecular modeling, most of the compounds proved to be poorly active. However, strategies for restoring activity within this series of novel chemotypes were discovered and crucial structure-activity relationships were deduced. The compounds presented may serve as starting point for developing novel JAK inhibitors and as a valuable training set for in silico models.
Gehringer, Matthias,Forster, Michael,Pfaffenrot, Ellen,Bauer, Silke M.,Laufer, Stefan A.
p. 2516 - 2527
(2015/08/24)

THE PRESENT INVENTION RELATES TO PROCESS FOR THE PREPARATION OF TOFACITINIB AND INTERMEDIATES THEREOF.
The present invention relates to process for the preparation of tofacitinib and intermediates thereof.
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(2014/07/21)

Asymmetric total synthesis of Tofacitinib
A novel stereoselective synthesis of Tofacitinib (CP-690,550), a Janus tyrosine kinase (JAK3) specific inhibitor, has been achieved starting from (5S)-5-hydroxypiperidin-2-one in 10 steps from 2 with a 9.5% overall yield. The potentiality of this synthetic route is the obtention of tert-butyl-(3S,4R)-3- hydroxy-4-methylpiperidine-1-carboxylate (6b) as a new chiral precursor involved in the synthesis of CP690,550, in a three-step reaction, without epimerizations, rather than the 5 or more steps used in described reactions to achieve this compound from analogues of 6b.
Maricán, Adolfo,Simirgiotis, Mario J.,Santos, Leonardo S.
supporting information
p. 5096 - 5098
(2013/09/02)

PIPERIDINE INHIBITORS OF JANUS KINASE 3
The present invention relates to a new piperidine inhibitors of Janus Kinase 3 activity, pharmaceutical compositions thereof, and methods of use there-of.
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Page/Page column 53-54

(2010/11/05)

THERAPEUTIC AGENTS
The invention provides a compound of formula (I): wherein R1, and W have any of the values defined in the application; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).
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Page/Page column 62

(2010/04/03)

COMBINATION THERAPIES FOR RHEUMATOID ARTHRITIS
This disclosure relates to pharmaceutical combination therapies for the treatment or prevention of arthritis, such as rheumatoid arthritis, in a human comprising a Janus Kinase inhibitor or a pharmaceutically acceptable salt thereof and at least one anti-arthritic agent or a pharmaceutically acceptable salt thereof. This disclosure also relates to certain methods for treating or preventing arthritis, such as rheumatoid arthritis, in a human comprising co-administering to a human a Janus Kinase inhibitor or a pharmaceutically acceptable salt thereof and at least one anti-arthritic agent or a pharmaceutically acceptable salt thereof.
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Page/Page column 52

(2010/11/30)

Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino) piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)
Here, we examine the significance that stereochemistry plays within the clinically relevant Janus kinase 3 (Jak3) inhibitor 1 (CP-690,550). A synthesis of all four enantiopure stereoisomers of the drug was carried out and an examination of each compound revealed that only the enantiopure 3R,4R isomer was capable of blocking Stat5 phosphorylation (Jak3 dependent). Each compound was profiled across a panel of over 350 kinases, which revealed a high level of selectivity for the Jak family kinases for these related compounds. Each stereoisomer retained a degree of binding to Jak3 and Jak2 and the 3R,4S and 3S,4R stereoisomers were further revealed to have binding affinity for selected members of the STE7 and STE20 subfamily of kinases. Finally, an appraisal of the minimum energy conformation of each stereoisomer and molecular docking at Jak3 was performed in an effort to better understand each compounds selectivity and potency profiles.
Jiang, Jian-Kang,Ghoreschi, Kamran,Deflorian, Francesca,Chen, Zhi,Perreira, Melissa,Pesu, Marko,Smith, Jeremy,Nguyen, Dac-Trung,Liu, Eric H.,Leister, William,Costanzi, Stefano,O'Shea, John J.,Thomas, Craig J.
supporting information; experimental part
p. 8012 - 8018
(2009/12/07)

PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES; THEIR INTERMEDIATES AND SYNTHESIS
This invention relates to methods and intermediates useful for the synthesis of pyrrolo [2,3-d] pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3- {(3R, 4R)-4-methyl-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
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Page/Page column 22-23

(2010/11/25)

Chiral salt resolution
A method for resolving enantiomers of a compound containing the structure of the formula: 1wherein R4or R5 may contain one or more asymmetric centers, by mixing a racemic mixture of enantiomers of a compound, containing the structure of said formula; in a solvent, with a resolving compound having a defined stereospecificity, to form a solution and with said resolving agent being capable of binding with at least one but not all of said enantiomers to form a precipitate, containing said at least one of said enantiomers in stereospecific form and collecting either the precipitate and purifying it or collecting the solution with contained other of said enantiomers and recrystallizing the enantiomer contained in said solution.
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(2008/06/13)

Chemical Properties

Density: 1.198 g/cm³
Solubility:Aqueous Acid (Slightly), Methanol (Slightly), Water (Slightly, Heated)
Storage Temp.:2-8°C(protect from light)
Refractive Index: 1.636
PKA: 13.36±0.50(Predicted)
PSA: 56.84000
LogP: 1.72090

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477600-74-1

Articles about 477600-74-1Total 38 be found

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Chemical Properties

Density: 1.198 g/cm³

Solubility:Aqueous Acid (Slightly), Methanol (Slightly), Water (Slightly, Heated)

Storage Temp.:2-8°C(protect from light)

Refractive Index: 1.636

PKA: 13.36±0.50(Predicted)

PSA: 56.84000

LogP: 1.72090

Global suppliers and manufacturers of 477600-74-1total 124 suppliers on LookChem

Article Database

477600-74-1

Articles about 477600-74-1Total 38 be found

More Articles about upstream products of 477600-74-1

More Articles about downstream products of 477600-74-1

Chemical Properties

Density: 1.198 g/cm3

Solubility:Aqueous Acid (Slightly), Methanol (Slightly), Water (Slightly, Heated)

Storage Temp.:2-8°C(protect from light)

Refractive Index: 1.636

PKA: 13.36±0.50(Predicted)

PSA: 56.84000

LogP: 1.72090

Global suppliers and manufacturers of 477600-74-1total 124 suppliers on LookChem

Density: 1.198 g/cm³