专利号:US-11866398-B2 优先权日:2018-05-15 标 题:Total synthesis of prostaglandin J natural products by stereoretentive metathesis 发明人:LI JIAMING; CHEN XU; AHMED TONIA S; STOLTZ BRIAN M; GRUBBS ROBERT H 权利人:CALIFORNIA INST OF TECHN 摘要:This invention relates generally to the synthesis of Δ12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. Δ12-Prostaglandin J products were generated with excellent selectivity (>99% Z) and in moderate to high/good yields (47% to 80% yield; 58% to 80% yield).
专利号:WO-2025078505-A1 优先权日:2023-10-13 标 题 :One pot gmp scalable production method for the synthesis of dextran-guanidine-bisphosphonate conjugate 发明人:HOLMBERG ANDERS R 权利人:DEXTECH MEDICAL AB 摘要:The disclosure relates to a large scale GMP synthesis of a modified dextran conjugate, and more particularly to a dextran-guanidine-bisphosphonate conjugate wherein the bisphosphonate is an alendronate group. The disclosure relates to a large scale GMP synthesis that produces high purity, pharmaceutical grade dextran-guanidine-bisphosphonate conjugate. The present disclosure further concerns the use of said dextran-guanidine-bisphosphonate conjugate in medicines treating tumors.
专利号:US-10918627-B2 优先权日:2016-05-11 标 题:Convergent and enantioselective total synthesis of Communesin analogs 发明人:MOVASSAGHI MOHAMMAD; LATHROP STEPHEN PAUL; POMPEO MATTHEW W; CHANG WEN-TAU TIMOTHY 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A highly convergent biomimetic synthesis of a complex polycyclic scaffold has been successfully implemented. From these efforts, compounds having a structure of Formula (I): n nor a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R 1 -R 8 and m, n, r, s, t, and u are as defined herein, is provided. Methods of making such compounds are also disclosed as are methods for the treatment of cancer, various infectious diseases, and abnormal cardiovascular function.
专利号:US-6620942-B2 优先权日:1998-12-23 标题 :Synthesis of histamine dihydrochloride 发明人:YEH WEN-LUNG; ANTCZAK CASIMIR; MCGOLRICK JEFFRY DAVID; ROTH MICHAEL JOSEPH; WRONA MARK 权利人:MAXIM PHARMACEUTICALS 摘要:The invention disclosed herein relates to the preparation of pharmaceutical grades of histamine dihydrochloride using a two step non-enzymatic synthetic method. The invention disclosed herein describes the synthesis of histamine dihydrochloride by the non-enzymatic decarboxylation of histidine and the step-wise conversion of the decarboxylated product to the dihydrochloride salt form. The invention disclosed herein considers a final product of histamine dihydrochloride containing less than each of the following: 0.8% L -histidine HCl monohydrate, 0.1% individual chromatographic impurities, and 2% total impurities, to be acceptable for pharmaceutical use.
专利号:US-6770763-B2 优先权日:2002-06-11 标题 :Asymmetric synthesis of amino-pyrrolidinones 发明人:MAGNUS NICHOLAS A; CONFALONE PASQUALE N; SAVAGE SCOTT A; YATES MATTHEW; WALTERMIRE ROBERT E; MELONI DAVID J; CAMPAGNA SILVIO 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described.These compounds are useful as intermediates for MMP and TACE inhibitors.
专利号:US-4958037-A 优先权日:1985-07-29 标题 :Precursors and synthesis of methyl-9-oxo-11α, 16-dihydroxy-16-vinyl-5-cis-13-trans-prostadienoates 发明人:FLOYD JR MIDDLETON B 权利人:AMERICAN CYANAMID CO 摘要:Novel precursors for the synthesis of methyl-9-oxo-11 alpha ,16-dihydroxy-16-vinyl-5-cis-13-trans prostadienoates having the formulae (2) (3) (4a) (4b) wherein R1 is H or C1-C4 alkyl; R2 is C1-C4 alkyl, R3 is H, C1-C4 trialkylsilyl or C1-C6 alkyl; X1 is halogen, cyano, C1-C4 alkoxycarbonyl, carboxy or tri (C1-C4 alkoxy)methyl; n is 2-4 inclusive; and P1 is H or a blocking or protective group; congeners and racemic mixture of these compounds and processes of synthesizing them.
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