专利号:US-5670666-A 优先权日:1993-09-27 标题:Process for preparing intermediates for the synthesis of D1 antagonists 发明人:HOU DONALD; DRAPER RICHARD W; LEE GARY M; MAS JANET L 权利人:SCHERING CORP 摘要:Disclosed are a process and intermediates of the formulae ##STR1## wherein X - is halide, BF 4 - , R 3 SO 3 - , wherein R 3 is C 1 -C 6 alkyl, CF 3 , C 1 -C 6 alkylphenyl or phenyl, and Q is a group of the formula ##STR2## wherein R is C 1 -C 6 alkyl; useful for preparing benzazepine intermediates of the formula ##STR3## These benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.
专利号:US-7186709-B2 优先权日:2002-08-27 标 题:Dihydropyrancarboxamides and uses thereof 发明人:SCHREIBER STUART L; STAVENGER ROBERT A; MITCHISON TIMOTHY J; MALIGA ZOLTAN 权利人:HARVARD COLLEGE 摘要:The present invention provides novel dihydropyrancarboxamide compounds of formula (I): n nand collections of these compounds, and provides methods for the synthesis of these compounds; wherein R 1 –R 6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
专利号:US-9035061-B2 优先权日:2010-07-13 标题:Process for preparing a biphenyl-2-ylcarbamic acid 发明人:COLSON PIERRE-JEAN 权利人:COLSON PIERRE-JEAN; THERAVANCE BIOPHARMA R & D IP LLC 摘要:The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.
专利号:US-7385064-B1 优先权日:2005-11-30 标题 :Catalysts for use in enantioselective synthesis 发明人:DAVIES HUW M L; REDDY RAVISEKHARA P 权利人:UNIV NEW YORK STATE RES FOUND 摘要:Disclosed are compounds having the following formula: n nin which Z 11 is selected from a substituted or unsubstituted saturated adamantyl or other polycyclic group and a substituted or unsubstituted branched acyclic group containing at least 5 carbon atoms at least one of which is a tertiary carbon; and in which Z 12 is a cyclic imide. Methods of using these compounds as chiral catalysts for carbenoid reactions and for enantioselective C—H aminations are also described.
专利号:WO-9509156-A1 优先权日:1993-09-27 标 题 :Processes and intermediates for the enantiospecific synthesis of benzo(d)naphth(2.1-b)azepines
专利号:US-9351954-B2 优先权日:2009-12-04 标 题:Multicyclic compounds and methods of use thereof 发明人:SHAO LIMING; CAMPBELL JOHN EMMERSON; HEWITT MICHAEL CHARLES; CAMPBELL UNA; HANANIA TALEEN G 权利人:SUNOVION PHARMACEUTICALS INC; PGI DRUG DISCOVERY LLC 摘要:Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. For example, disclosed herein are compounds having formula (IIa) shown below, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein the variables are defined herein. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
摘要:Scholz, U.; Dong, W.; Feng, J.; Shi, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 98. 摘要:Martin, A. R., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 170. 摘要:Giel, M.-C.; Smedley, C. J.; Moses, J. E., Science of Synthesis, (2021) , 442. 摘要:Yoshikai, N., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) .