专利号:WO-2021038581-A1 优先权日:2019-08-30 标题 :A one step synthesis of 2-substituted benzo[b]thiophenes 发明人:SEKAR GOVINDASAMY; POONGUZHALI ELAMVAZHUTHI 权利人:INDIAN INST TECH MADRAS 摘要:The invention pertains to a one step synthesis of 2-substituted benzo[ b ]thiophene of general formula wherein the synthesis of 2-substituted benzo[ b ]thiophenes is by reacting the starting materials substituted or unsubstituted 2-halogenobenzaldehyde and substituted or unsubstituted acetyl/phenacyl bromide with a catalyst, a sulphur source and phase transfer catalyst in an aqueous medium with atmospheric air and at temperature in the range of 25°C-30°C.
专利号:US-9150840-B2 优先权日:2011-08-26 标题 :Isolated bacterial strain of Achromobacter sp. MTCC 5605 and a highly enantioselective epoxide hydrolase isolated therefrom 发明人:KAMAL AHMED; KHANNA ROHINI; KUMAR CHITYAL GANESH; SHAIK ANVER BASHA; KUMAR MATAM SHIVA 权利人:KAMAL AHMED; KHANNA ROHINI; KUMAR CHITYAL GANESH; SHAIK ANVER BASHA; KUMAR MATAM SHIVA; COUNCIL SCIENT IND RES 摘要:The present invention relates to a novel epoxide hydrolase enzyme which aims to achieve a high degree of resolution towards a broader range of substrates with high enantioselectivity and yields with minimal product inhibition. The invention further relates to a new bacterial strain Achromobacter sp. MTCC 5605 isolated from a petroleum-contaminated sludge sample, capable of producing the said enzyme. It is notable that the enzyme can be used as whole bacterial cell preparation, which allows continuous hydrolysis of substrates at even higher concentration and have an advantage of being recycled. The invention further relates to a process for the hydrolysis of different aryl epoxides which are potential synthons of intermediates for the synthesis of chiral amino alcohols and bioactive compounds like β-blockers.
专利号:US-8101633-B2 优先权日:2006-06-05 标 题 :Preparation and utility of substituted imidazopyridine compounds with hypnotic effects 发明人:GANT THOMAS G; SARSHAR SEPEHR 权利人:GANT THOMAS G; SARSHAR SEPEHR; AUSPEX PHARMACEUTICALS INC 摘要:The present disclosure is directed to modulators of GABA A receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of sleep disorders and/or for providing a patient in need with a hypnotic, anxiolytic or anti-convulsive effect are described.
专利号:US-8906915-B2 优先权日:2009-12-17 标 题:Compounds, compositions, and methods for controlling biofilms 发明人:DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S 权利人:DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S; UNIV LEUVEN KATH 摘要:The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.
专利号:US-8829014-B2 优先权日:2006-04-07 标题 :Thiazole and thiophene analogues, and their use in treating autoimmune diseases and cancers 发明人:GIORDANO ANTHONY; VASU KAMALA K; THAKAR HARDIK M; GIRI RAJAN S; SUDARSANAM VASUDEVAN; YERANDE SWAPNIL G; INAMDAR GAJANAN S 权利人:GIORDANO ANTHONY; VASU KAMALA K; THAKAR HARDIK M; GIRI RAJAN S; SUDARSANAM VASUDEVAN; YERANDE SWAPNIL G; INAMDAR GAJANAN S; UNIV LOUISIANA STATE; PATEL PHARMACEUTICAL EDUCATION & RES DEV PERD CT B V 摘要:Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.
专利号:CN-107686481-A 优先权日:2017-09-28 标题:A method for ultrasonic solvent-free synthesis of thiazole derivatives containing acetophenone triazole groups
[参考文献]: Miroslav Soural, Et Al. Efficient Solid-Phase Synthesis Of 2-Substituted-3-Hydroxy-4(1H)-Quinolinone-7-Carboxamides With Two Diversity Positions. J Comb Chem. 2007 Sep-Oct;9(5):793-6.
合成参考文献
摘要:Lipshutz, B. H.; Ghorai, S., Science of Synthesis Knowledge Updates, (2014) 2, 178. 摘要:Hou, X.-L.; Peng, X.-S.; Yeung, K.-S.; Wong, H. N. C., Science of Synthesis Knowledge Updates, (2011) 2, 285. 摘要:Hou, X.-L.; Peng, X.-S.; Yeung, K.-S.; Wong, H. N. C., Science of Synthesis Knowledge Updates, (2011) 2, 263. 摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2010) 1, 431. 摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2010) 1, 428.