N-(Tert-Butyloxycarbonyl)-O-Benzyl-L-Serinol置于镍 Sodium Hydride,三乙胺体系中,用 四氢呋喃,乙醇,二氯甲烷,水 用作溶剂,化学反应生成N-Boc-D-丙氨醇 参考文献:Conversion Of Chiral Amino Acids To Enantiomerically Pure α-Methylamines 标题:Conversion Of Chiral Amino Acids To Enantiomerically Pure α-Methylamines 摘要:Enantiomerically Enriched Alpha-Methylamines Are Obtained In High Yield By Raney Nickel Reduction Of N-Boc-Protected,Amino Acid-Derived Thioethers. Doi:10.1016/0040-4039(95)00039-F
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-11993577-B2 优先权日:2021-09-01 标 题 :Synthesis of MDMA or its optically active (R)- or (S)-MDMA isomers 发明人:FAWAZ MAJED; MORRA NICHOLAS 权利人:EMPATHBIO INC 摘要:Provided herein is a process for the preparation of 3,4-methylenedioxymethamphetamine, (R)-3,4-methylenedioxymethamphetamine and (S)-3,4-methylenedioxymethamphetamine.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2018016227-A1 优先权日:2015-02-03 标题:Process for the synthesis of difluoromethyl ether-based compounds 发明人:SLASSI ABDELMALIK; DOVE PETER 权利人:TRILLIUM THERAPEUTICS INC 摘要:The present application relates to a novel process for the preparation of difluoromethyl ether-based derivatives from, for example, aliphatic and aromatic hydroxyl precursors, compositions comprising these compounds and their use, in particular as precursors for medicines for the treatment of diseases, disorders or conditions. In particular, the present application includes the process of preparing compounds of Formula (I), and compositions and uses thereof:
专利号:US-2024174678-A1 优先权日:2020-06-30 标 题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
专利号:US-2024217919-A1 优先权日:2021-04-09 标题:Novel methods for synthesizing enantiopure (s)-methadone, (r)-methadone, racemic (r,s)-methadone and related analogue substances 发明人:MANFREDI PAOLO L; INTURRISI CHARLES E; MATTAREI ANDREA; BANZATO MARCO; FURLAN ALBERTO; ONGARO ALBERTO; HEASLEY BRIAN H; TUCKER ZACHARY D 权利人:MANFREDI PAOLO L; INTURRISI CHARLES E 摘要:Methods for the synthesis of enantiopure (S)-methadone, (R)-methadone, (R,S)-methadone and related analogues starting from optically active or racemic N-substituted cyclic sulfamidates, or N-substituted aziridines with retention of stereochemical configuration. The methods avoid the formation of isomethadone-nitrile by-products observed under the previously reported conditions, namely the ring-opening reaction of the corresponding 1,1,2-trimethylaziridin-1-ium salt and the 2,2-diphenylacetonitrile anion, resulting in improved yields and facile purification operations.