- Preparation method of SGLT2 inhibitor-empagliflozin
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The invention relates to a preparation method of a SGLT2 inhibitor-empagliflozin. The preparation method includes: using 2-methylaniline as a starting raw material, subjecting the starting raw material to bromination, diazotization, chlorination and bromination, and enabling the starting raw material to be in friedel-crafts alkylation reaction with (S)-3-phenoxy tetrahydrofuran to obtain an intermediate-(S)-3-(4-(5-bromo-2-chlorobenzyl)phenoxy) tetrahydrofuran; subjecting the intermediate and 2, 3, 4, 6-tetra-O-trimethylsilyl-D-glucolactone to condensation, etherification and methoxy removal.The preparation method has the advantages that compared with existing synthetic methods, 2-methylaniline is used as the starting raw material, so that the raw material is low in cost and easy to get,the process is easy for industrialization, and a synthetic route is short and easy to operate; in the process of preparation, temperature conditions are easy to control, reaction conversion rate is high, and total yield is up to higher than 75%. In addition, through the preparation method, the inhibitor is less prone to isomerization, impurities are few, and purity of the inhibitor can be improvedto higher than 99%.
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Paragraph 0015; 0018
(2018/03/26)
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- NOVEL 2-AMINO-PYRIDINE AND 2-AMINO-PYRIMIDINE DERIVATIVES AND MEDICINAL USE THEREOF
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Provided is a compound superior in an autotaxin inhibitory action and the like, effective as a prophylactic or therapeutic drug for diseases involving ATX. The present invention relates to a compound represented by the following formula (I): [wherein each symbol is as described in the DESCRIPTION], which has a superior autotaxin inhibitory action and is useful as a prophylactic or therapeutic drug for diseases involving ATX.
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Paragraph 0476-0477
(2017/03/14)
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- 5-bromo-2-chloro -4 the-oxethyl diphenylmothane [...] preparation method
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The invention relates to the chemical field and particularly relates to a novel synthesis method for preparing a key intermediate 5-bromine-2-chlorine-4'-ethyoxyl diphenylmethane of a drug dapagliflozin for treating diabetes mellitus II. The preparation method comprises the following steps: enabling a starting raw material ortho-toluidine to firstly perform bromization and then perform chlorination after diazotization on a benzene ring with N-bromo-succinimide; then, in the presence of a halogenating agent, performing halogenating reaction of beta-position; and finally, performing Friedel-Crafts alkylation synthesis with phenetole, thereby obtaining the key intermediate. The preparation method is simple and convenient, economical and relatively high in reaction yield in each step, and suitable for industrial production.
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Paragraph 0029-0030
(2017/04/03)
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- Iterative Reductive Aromatization/Ring-Closing Metathesis Strategy toward the Synthesis of Strained Aromatic Belts
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The construction of all sp2-hybridized molecular belts has been an ongoing challenge in the chemistry community for decades. Despite numerous attempts, these double-stranded macrocycles remain outstanding synthetic challenges. Prior approaches
- Golder, Matthew R.,Colwell, Curtis E.,Wong, Bryan M.,Zakharov, Lev N.,Zhen, Jingxin,Jasti, Ramesh
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supporting information
p. 6577 - 6582
(2016/06/09)
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- STROBILURIN TYPE COMPOUNDS FOR COMBATING PHYTOPATHOGENIC FUNGI
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The present invention relates to novel strobilurine type compounds, to compositions comprising at least one such compound, to methods for combating phytopathogenic fungi, to the use of such compounds and to seeds coated with at least one such compound. (I
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Page/Page column 107
(2015/01/16)
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- RENIN INHIBITORS
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Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency, wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R1 is hydrogen, C1-6 -alkyl or C3-6 -cycloalkyl, wherein said C1-6 -alkyl or C3-6 -cycloalkyl group can be independently substituted with 1-3 halogens; A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to another five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is a bond or -(C=O)-, -CH(OH)-, -CH2- or =CH-; U is a bond or -CH2-, or for the case when V is =CH-, U is -CH=; X is =CH-, =CF-, =C(OR3)-, or -C=O-; and Y is =CH-, =CF-, =N-, or for the case when X is -C=O-, Y is -N(R3)-.
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Page/Page column 24
(2011/04/13)
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- METHYL SULFANYL PYRMIDMES USEFUL AS ANTIINFLAMMATORIES, ANALGESICS, AND ANTIEPILEPTICS
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The present invention relates to pyrimidine derivatives of Formula (Ia) and (Ib) (including tautomers, isomers, prodrugs, and pharmaceutically acceptable salts thereof). Said compounds are useful in the treatment of pain (such as neuropathic pain), inflammation, and epilepsy (by acting as anticonvulsants). Methods of medical treatment making use of said compounds, as well as additional compounds of Formula (IIa) and (IIb), are also disclosed.
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Page/Page column 110
(2010/12/18)
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- Substituted 4-Amino-Quinazoline Compounds with Metabotropic Glutamate Receptor Regulating Activity and Uses Thereof
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Substituted 4-amino-quinazoline compounds corresponding to formula I methods for their production, pharmaceutical compositions containing these compounds as active agents, and the uses thereof for treating or inhibiting disorders or disease states.
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Page/Page column 77; 78
(2009/04/24)
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- GLUCOPYRANOSYL-SUBSTITUTED DIFLUOROBENZYL-BENZENE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR MANUFACTURE
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Glucopyranosyl-substituted difluorobenzyl-benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention
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Page/Page column 36
(2010/11/30)
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- Glucopyranosyl-substituted ((hetero)cycloalkylethynyl-benzyl)-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
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Glucopyranosyl-substituted ((hetero)cycloalkylethynyl-benzyl)-benzene derivatives of the general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
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Page/Page column 19
(2010/11/25)
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- Processes for preparing of glucopyranosyl-substituted (ethynyl-benzyl)-benzene derivatives and intermediates thereof
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The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1, R2 and R3 are defined according to claim 1 and to intermediates of said processes.
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Page/Page column 25-26
(2010/11/26)
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- Heck, direct arylation, and hydrogenation: Two or three sequential reactions from a single catalyst
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Palladium-catalyzed tandem multifunctional reactions leading to the synthesis of substituted biaryl molecules have been developed including tandem Heck-direct arylation and tandem-sequential Heck-direct arylation-hydrogenation. These reactions occur in go
- Leclerc, Jean-Philippe,Andre, Mathieu,Fagnou, Keith
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p. 1711 - 1714
(2007/10/03)
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- Glucopyranosyl-substituted ((hetero)arylethynyl-benzyl)-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
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Glucopyranosyl-substituted (hetero)arylethynyl-benzene derivatives of the general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
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Page/Page column 20
(2008/06/13)
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- D-xylopyranosyl-phenyl-substituted cycles, medicaments containing such compounds, their use and process for their manufacture
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D-Glucopyranosyl-phenyl-substituted cycles of general formula I wherein the groups R1 to R6, Z, Cy and R7a, R7b, R7c, R7d are defined as in claim 1, have an inhibiting effect on the sodium-dependent glucose cotransporter SGLT. The present invention also relates to pharmaceutical compositions for the treatment of metabolic disorders.
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Page/Page column 20
(2010/02/15)
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- Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein
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The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.
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Page/Page column 22
(2010/11/24)
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- INDAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF
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The present invention can provide a cancer treatment drug containing, as an active ingredient, a substance selected from the group consisting of an indazole compound of the following formula (I), a pharmaceutically acceptable salt, a hydrate, a water adduct and a solvate:
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Page/Page column 26
(2010/11/24)
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- Glucopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture
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Glucopyranosyl-substituted benzene derivatives of general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined herein and the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
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Page/Page column 21-22
(2008/06/13)
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- GLUCOPYRANOSYL-SUBSTITUTED BENZOL DERIVATIVES, DRUGS CONTAINING SAID COMPOUNDS, THE USE THEREOF AND METHOD FOR THE PRODUCTION THEREOF
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The invention relates to glucopyranosyl-substitutedted benzol derivatives of general formula (I), wherein rests R1 to R6 and R7a, R7b, R7c are such as defined in the claim 1, including the tautomers, stereoisomers, mixtures and the salts thereof. The inventive compounds are useful for treating metabolic diseases.
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Page/Page column 53
(2008/06/13)
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- Triazolone derivatives, use thereof, and intermediates therefor
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Triazolone derivatives represented by the formula wherein R1represents optionally substituted C1-10alkyl, A1—L1—, A1—ON═CA2, etc.; R2represents hydrogen, C1-6alkyl, etc.; R3represents C1-6alkoxy, etc.; one of T, U, and V represents CR4, another represents CH or nitrogen, and the remaining one represents CR5or nitrogen; and W represents CR6or nitrogen.
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- 3-Arylpiperidines as potentiators of existing antibacterial agents
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Important resistance patterns in Gram-negative pathogens include active efflux of antibiotics out of the cell via a cellular pump and decreased membrane permeability. A 3-arylpiperidine derivative (1) has been identified by high-throughput assay as a pote
- Thorarensen, Atli,Presley-Bodnar, Alice L.,Marotti, Keith R.,Boyle, Timothy P.,Heckaman, Charlotte L.,Bohanon, Michael J.,Tomich, Paul K.,Zurenko, Gary E.,Sweeney, Michael T.,Yagi, Betty H.
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p. 1903 - 1906
(2007/10/03)
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- Phenylacetylene derivatives and agricultural/horticultural fungicides
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A phenylacetylene derivative represented by the formula [I]: {wherein X is a halogen atom, a C1-C6alkyl group, a C2-C6alkoxy group, a C2-C6haloalkyl group, etc., n is 0 or an integer of fro
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- Fullerene tectonics. Part 2. Synthesis and pyrolysis of halogenated benzo[c]phenanthrenes
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Halogenated benzo[c]phenanthrenes with a halogen in the hindered fiord region are prepared by the photochemical cyclisation of appropriately substituted stilbenes. Pyrolysis gives the corresponding benzo[ghi]fluoranthrenes in moderate yields. At higher temperatures a competing rearrangement pathway to cyclopenta[cd]pyrene occurs.
- Plater, M. John
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p. 2903 - 2909
(2007/10/03)
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