专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-7102023-B2 优先权日:1999-11-24 标 题:Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 发明人:BUCHWALD STEPHEN L; PLANTE OBADIAH J; SEEBERGER PETER H 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
专利号:US-10793495-B2 优先权日:2015-08-14 标 题:Synthesis of polyaryl substituted aryl compounds 发明人:BOULOS RAMIZ; FEUTRILL JOHN 权利人:BOULOS & COOPER PHARMACEUTICALS PTY LTD 摘要:A method for the synthesis of a aryl compound of Formula (1).n nU T-W—R 1 ) n    (1)
专利号:US-8283476-B2 优先权日:2007-06-26 标 题:Transition metal catalyzed synthesis of 2H-indazoles 发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; RKYEK OMAR; URMANN MATTHIAS 权利人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; RKYEK OMAR; URMANN MATTHIAS; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.
专利号:WO-2024073221-A1 优先权日:2022-09-29 标题:Synthesis of palladium(0) phosphine complexes 发明人:MACQUEEN PRESTON; GHORAI SUBIR; COLACOT THOMAS 权利人:SIGMA ALDRICH CO LLC 摘要:Provided is an optimized process for the synthesis of palladium(O) phosphine complexes. The process described herein is characterized by a more efficient reaction control, high yield and purity, the use of readily available starting materials, and savings in reaction time and steps, thereby offering increased sustainability when compared to processes reported in the state of the art.
专利号:US-8026375-B2 优先权日:2007-04-13 标题:Transition metal catalyzed synthesis of N-aminoindoles 发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; RKYEK OMAR; URMANN MATTHIAS; ALONSO JORGE 权利人:SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要:L794: Wikipedia. Palladium. Last Updated 14 June 2009. 摘要:L798: International Programme on Chemical Safety (IPCS) INCHEM (2002). Environmental Health Criteria for Palladium. 摘要:A21: Smith DR, Kahng MW, Quintanilla-Vega B, Fowler BA: High-affinity renal lead-binding proteins in environmentally-exposed humans. Chem Biol Interact. 1998 Aug 14;115(1):39-52.