- ETHYNYL COMPOUNDS, THEIR PREPARATION AND THEIR THERAPEUTIC USE FOR THE TREATMENT OF MALARIA
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The present disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R1 means a fluorine atom or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms; R2 means a chlorine atom, a linear alkyl radical containing 1, 2 or 3 carbon atoms or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms, and R means a hydrogen atom or a radical of formula (la). The present disclosure also relates to processes for their preparation as well their therapeutic uses, in particular such as for use in the treatment of malaria.
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Page/Page column 44
(2019/01/21)
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- METHOD FOR PRODUCING HALOGENATED BENZENE DERIVATIVE
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PROBLEM TO BE SOLVED: To provide a method for producing a halogenated benzene derivative, which is highly efficient and economically advantageous. SOLUTION: The method produces a halogenated benzene derivative represented by formula (2) by reacting a benzene derivative represented by formula (1) with a halogenating agent selected from N-halogen succinimide and the like in the presence of an acid selected from sulfuric acid and methanesulfonic acid. (R1 is H, a hydroxyl group, or an alkoxy group; R2 and R3 are each independently H or a hydrocarbon group; a is an integer of 1-4; b is an integer of 1-4; a+b is an integer of 2-5; X is a halogen atom; c is an integer of 1-4; and a+b+c is an integer of 3-6). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
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Paragraph 0075; 0076; 0077; 0078; 0079; 0080; 0081-0088
(2018/06/30)
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- METHOD FOR PRODUCING HALOGEN COMPOUND
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PROBLEM TO BE SOLVED: To provide a method for producing an iodine compound with high efficiency and in an economically advantageous manner. SOLUTION: According to a method, in the presence of at least one acid selected from sulfuric acid, methane sulfonic acid, and trifluoromethane sulfonic acid, and an oxidizing agent, a benzene derivative is reacted with at least one halogenating agent selected from hydrogen halide and haloid, to produce a halogen compound of a corresponding benzene derivative. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
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Paragraph 0084; 0085; 0088; 0089; 0090; 0091; 0092; 0094
(2018/07/03)
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- Synthesis method of 2-methyl-5-iodobenzoic acid
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The invention discloses a synthesis method of 2-methyl-5-iodobenzoic acid. The synthesis method includes: using air as an oxidant and elemental iodine as an iodo reagent for catalytic oxidation to prepare 2-methyl-5-iodobenzoic acid. The synthesis method specifically includes: using o-toluic acid as a raw material, dissolving the raw material in a reaction solvent, adding the elemental iodine, inorganic protonic acid and catalyst, and using air for catalytic oxidation reaction for 6-48h at reaction temperature of 0-120 DEG C to obtain 2-methyl-5-iodobenzoic acid. Oxygen in the air is utilizedto complete catalytic oxidation, so that cost is lowered obviously; reaction yield is 85-95%, and purity is up to 99%; equipment and instruments needed for reaction are simple and easy to operate, andthe synthesis method is convenient in aftertreatment operation, high in safety and suitable for industrial production.
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Paragraph 0054-0098
(2018/03/28)
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- N-Iodosuccinimide (NIS) in Direct Aromatic Iodination
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N-Iodosuccinimide (NIS) in pure trifluoroacetic acid (TFA) offers a time-efficient and general method for the iodination of a wide range of mono- and disubstituted benzenes at room temperature, as demonstrated in this paper. The starting materials were generally converted into mono-iodinated products in less than 16 hours at room temperature, without byproducts. A few deactivated substrates needed addition of sulfuric acid to increase the reaction rate. Another exception was methoxybenzenes that preferentially were iodinated by NIS in acetonitrile with only catalytic amounts of TFA.
- Bergstr?m, Maria,Suresh, Ganji,Naidu, Veluru Ramesh,Unelius, C. Rikard
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p. 3234 - 3239
(2017/06/21)
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- Process for synthesizing card Geleg only (by machine translation)
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The invention discloses a process for synthesizing card Geleg only, in order to 2?Methyl benzoic acid as starting material, use of improvised catalyst, reaction to produce the iodine iodate a in the middle, or in 2?Methyl benzoic acid as starting material, the metal reagent and under the action of catalyst, by adding liquid bromine, synthetic intermediates b; optionally intermediate one or intermediate two acylation reaction with thionyl chloride, to Friedel-crafts reaction produce intermediate three; in order to ALPHA?D?Glucose as raw material, with the reaction protection of all hydroxyl after pivalyl chloride, and then with zinc bromide, trimethyl silane reaction produce intermediate four; three intermediate the intermediate body, connecting delivery into intermediate five; finally under acidic conditions to remove the acyl special fifth heavenly stem, produce the target compound. card Geleg only of the present invention new process for the synthesis of high yield, mild condition, safety and reliability, is suitable for industrial production, raw material is cheap and easy to obtain, it is beneficial to control the production cost. (by machine translation)
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Paragraph 0032; 0033
(2016/12/01)
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- COMPOUNDS AND METHODS FOR TREATING RESPIRATORY DISEASES
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Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).
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Page/Page column 28
(2011/11/12)
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- Structure-based design, synthesis, and biological evaluation of a series of novel and reversible inhibitors for the severe acute respiratory syndrome - Coronavirus papain-like protease
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We describe here the design, synthesis, molecular modeling, and biological evaluation of a series of small molecule, nonpeptide inhibitors of SARS-CoV PLpro. Our initial lead compound was identified via high-throughput screening of a diverse chemical library. We subsequently carried out structure - activity relationship studies and optimized the lead structure to potent inhibitors that have shown antiviral activity against SARS-CoV infected Vero E6 cells. Upon the basis of the X-ray crystal structure of inhibitor 24-bound to SARS-CoV PLpro, a drug design template was created. Our structure-based modification led to the design of a more potent inhibitor, 2 (enzyme IC50 = 0.46 μM; antiviral EC50 = 6 μM). Interestingly, its methylamine derivative, 49, displayed good enzyme inhibitory potency (IC50 = 1.3 μM) and the most potent SARS antiviral activity (EC50 = 5.2 μM) in the series. We have carried out computational docking studies and generated a predictive 3D-QSAR model for SARS-CoV PLpro inhibitors.
- Ghosh, Arun K.,Takayama, Jun,Aubin, Yoann,Ratia, Kiira,Chaudhuri, Rima,Baez, Yahira,Sleeman, Katrina,Coughlin, Melissa,Nichols, Daniel B.,Mulhearn, Debbie C.,Prabhakar, Bellur S.,Baker, Susan C.,Johnson, Michael E.,Mesecar, Andrew D.
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experimental part
p. 5228 - 5240
(2010/03/04)
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- Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone
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Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent small molecule Hsp90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human cancer cell lines in vitro, with IC50 values averaging 20 nM.
- Kung, Pei-Pei,Funk, Lee,Meng, Jerry,Collins, Michael,Zhou, Joe Zhongxiang,Catherine Johnson,Ekker, Anne,Wang, Jeff,Mehta, Pramod,Yin, Min-Jean,Rodgers, Caroline,Davies II, Jay F.,Bayman, Eileen,Smeal, Tod,Maegley, Karen A.,Gehring, Michael R.
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supporting information; experimental part
p. 6273 - 6278
(2009/08/15)
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- PROCESS FOR PRODUCING 5-IODO-2-METHYLBENZOIC ACID
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The present invention provides a process for producing 5-iodo-2-methylbenzoic acid through iodination of 2-methylbenzoic acid, the process including, as essential steps, a reaction step of iodinating 2-methylbenzoic acid in the presence of a microporous compound, iodine, an oxidizing agent, and acetic anhydride, and a purification step including sublimation, distillation, crystallization, or a combination of two or more of these. According to the present invention, 5-iodo-2-methylbenzoic acid, which is useful for producing functional chemicals such as drugs, can be produced at high purity and high yield in a simple manner. Since the production process includes a simple reaction step and a simple separation/purification step, the load of purification is mitigated. In addition, the microporous compound such as a zeolite catalyst which has been separated and recovered from the reaction mixture can be repeatedly employed after performing of a simple treatment. Thus, the production process ensures a long service life of catalysts and high efficiency.
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Page/Page column 6
(2008/06/13)
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- AMIDE RESORCINOL COMPOUNDS
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The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as HSP-90 inhibitors.
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- PROCESS FOR PRODUCTION OF IODINE COMPOUNDS AND PROCESS FOR PRODUCTION OF HIGH-PURITY 5-IODO-2-METHYLBENZOIC ACID
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Provided is a production method for an iodine compound in which iodine is reacted with a substrate in the presence of a porous material having a pore diameter of 500 nm or less or in the presence of the above porous material and an oxidizing agent and a production process for high purity 5-iodo-2-methylbenzoic acid comprising an iodination reaction step carried out by the above-mentioned, a crystal precipitation and separation step in which a product is precipitated by adding water or cooling and then separated and a purification step in which crystal separated is recrystallized using an organic solvent. According to the production method for an iodine compound described above, iodine can be introduced into various substrates at a high selectivity. Since expensive metals and specific reagents do not have to be used, it can readily be carried out in an industrially scale, and the product having a high purity can be obtained. Further, the process comprising the iodination reaction, separation and purification steps described above makes it possible to readily obtain at a high yield, 5-iodo-2-methylbenzoic acid having a high purity which is useful in uses for functional chemical products such as medicines. The process of the present invention comprising iodination reaction, separation and purification steps is characterized by that it is simple in terms of a procedure and that the purification load is smaller, and it is very advantageous in industrially carrying out.
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Page/Page column 8
(2008/06/13)
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