专利号:US-6500955-B1 优先权日:2001-02-02 标 题:One pot synthesis of [2,8-Bis (trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, a mefloquine intermediate 发明人:CHAWLA HARMANDER PAL SINGH; JOHAR PERMINDER SINGH; MITTAL ALKA; MEENA RAM AVTAR; NEGI VILLENDRA SINGH 权利人:NAT INST OF PHARMACEUTICAL EDU 摘要:The present invention provides a simple single step process for the preparation of [2,8-bis(trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, comprising the step of condensing a halo-quinoline with an alpha-picolyl derivatives in the presence of a solvent, a base and a phase transfer catalyst at −10° C. to +90° C.
专利号:US-12275733-B2 优先权日:2016-11-07 标 题:Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders 发明人:GRETZKE DIRK; RITZELER OLAF; HEINELT UWE; WEHNER VOLKMAR; SCHMIDT FRIEDEMANN 权利人:SANOFI SA 摘要:The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
专利号:US-9440948-B2 优先权日:2010-09-03 标题:Nicotine compounds and analogs thereof, synthetic methods of making compounds, and methods of use 发明人:KEM WILLIAM READE; SOTI FERENC; ROUCHAUD ANNE; XING HONG; LINDSTROM JON; ANDRUD KRISTIN MARIE 权利人:KEM WILLIAM READE; SOTI FERENC; ROUCHAUD ANNE; XING HONG; LINDSTROM JON; ANDRUD KRISTIN MARIE; UNIV FLORIDA; UNIV PENNSYLVANIA 摘要:Embodiments of the present disclosure provide for compounds such as those shown in FIG. 1.1 (compounds A, B, C, and D), 2′substituted nicotine compounds, azetidine compounds, ether linked nicotine compounds (FIG. 1.2 , compounds E, F, G, and H), methods of synthesis of the compounds, methods of treatment of a condition using compounds A, B, C, D, 2′substituted nicotine compounds, azetidine compounds, or ether linked nicotine compounds, methods of selectively stimulating alpha7 nAChR and/or alpha4beta2 receptors, and the like.
专利号:US-8207337-B2 优先权日:2007-01-29 标 题:Reagent for organic synthesis reaction containing organic triol borate salt 发明人:MIYAURA NORIO; YAMAMOTO YASUNORI 权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD 摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).
专利号:CN-1370777-A 优先权日:2001-02-02 标题:Improved single-reactor synthesis of [2,8-di(trifluoromethyl)-4-quinolyl]-2-pyridyl methyl ketone and methylfluoro quine
专利号:US-2002188129-A1 优先权日:2001-02-02 标题:One pot synthesis of [2, 8-bis (trifluoromethyl)-4- quinolinyl]2-pyridinylmethanone, a mefloquine intermediate
摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 167. 摘要:Weibel, J.-M.; Blanc, A.; Pale, P., Science of Synthesis Knowledge Updates, (2018) 1, 19. 摘要:Wolf, C., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 885.