专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-2025188046-A1 优先权日:2023-12-08 标题:Ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent sufex connections via lithiated chemistry 发明人:KIM DONG-PYO; KANG JI-HO 权利人:POSTECH RES & BUSINESS DEV FOUND 摘要:Disclosed are ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent SuFEx connections via lithiated chemistry. In detail, a method of synthesizing an ortho-functionalized benzenesulfonyl fluoride derivative, the method comprises (a) reacting a benzenesulfonyl fluoride derivative represented by structural formula 1 with an organolithium represented by structural formula 2, thus synthesizing an intermediate represented by structural formula 3 in reaction scheme 1 and (b) reacting the intermediate with an electrophile, thus synthesizing a compound represented by structural formula 4 or a compound represented by structural formula 4′. The present disclosure enables the synthesis of several functionalized sulfonyl fluorides within a few seconds under mild temperature conditions in addition to the chemistry of Sulfonyl Fluoride Exchange (SuFEx), which is a next-generation click chemistry, so that sulfonyl fluoride, the main reactant of the SuFEx reaction, can be efficiently secured.
专利号:US-2011130591-A1 优先权日:2009-06-03 标 题:Steroselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; REEVES JONATHAN T; SONG JINHUA J 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for synthesis of a compound of Formula (X) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl,n wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; and n n R 2 and R 3 are each independently C 1 -C 5 alkyl.
专利号:US-11512062-B2 优先权日:2018-10-15 标 题:Process for the synthesis of piperazinyl-ethoxy-bromophenyl derivates and their application in the production of compounds containing them 发明人:BEAUREGARD LOUIS-PHILIPPE; BERTRAND MARTIAL; GIGUERE PASCALL; HARDOUIN CHRISTOPHE; SCHIAVI BRUNO 权利人:SERVIER LAB 摘要:Process for the industrial synthesis of the compound of formula (I):
专利号:US-2025002518-A1 优先权日:2023-06-16 标 题 :Synthesis of heteroarynes and use thereof 发明人:MATTMILLER ROBERTS COURTNEY COLLEEN; HUMKE JENNA NICOLE; QUINLIVAN ANSEL ANNABEL; BELLI ROMAN GIANCARLO; KARGBO SALLU SO; PLASEK ERIN ELIZABETH 权利人:UNIV MINNESOTA 摘要:Disclosed herein are heterocyclic arynes and methods for preparing the same. Heteroarynes such as 5-membered O- or N-heterocyclic arynes have been considered inaccessible due to ring strain associated with the triple bond. The methods described herein demonstrate that these arynes can be successfully prepared through the utility of pi-backbonding from a transition metal. Synthetic utility of this method has been demonstrated by the facile synthesis and functionalization of heterocycles using these heteroaryne building blocks.
专利号:US-2024010638-A1 优先权日:2020-11-13 标题:Improved synthesis of crac channel inhibitors 发明人:STAUDERMAN KENNETH; DUNN MICHAEL; OLMSTEAD KAY 权利人:CALCIMEDICA INC 摘要:Provided herein is an improved synthetic method for the production of CRAC channel inhibitors. The synthetic method provides a method for producing highly pure CRAC channel inhibitors for clinical testing.