(S)-3-Hydroxy-4-(P-Toluenesulfonyloxy)Butyronitrile置于镍 氢气体系中,用 乙醇 用作溶剂,化学反应生成(S)-3-吡咯烷醇 参考文献:Synthesis Of (3R)-Carboxy Pyrrolidine (A β-Proline Analogue) And Its Oligomer 标题:Synthesis Of (3R)-Carboxy Pyrrolidine (A β-Proline Analogue) And Its Oligomer 摘要:A Decamer Of A Beta-Amino Acid Analogue Of L-Proline,(3R)-Carboxy Pyrrolidine (Beta-Proline),Was Synthesized From A Readily Available (R)-Glycidol. It Was Found To Possess A Rigid Secondary Structure,As Evidenced By Its Cd Spectrum. The Beta-Proline Decamer,However,Failed To Bind To Profilin,Whereas The Corresponding Alpha-L-Proline Decamer Bound Tightly To This Protein. (C) 2000 Published By Elsevier Science Ltd. Doi:10.1016/s0960-894X(00)00486-8
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-7153960-B2 优先权日:2001-12-10 标 题:Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones 发明人:ZHOU JIACHENG; OH LYNETTE M; MA PHILIP; LI HUI-YIN; CONFALONE PASQUALE 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. n nThese compounds are useful as factor Xa inhibitors.
专利号:US-2024287084-A1 优先权日:2021-10-28 标 题 :Synthesis of [1,2,3]triazolo[4,5-d]pyrimidines 发明人:ADAM JEAN-MICHEL; GRETHER UWE; MOESSNER CHRISTIAN; TOSATTI PAOLO 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a process for the preparation of [1,2,3]triazolo[4,5-d]pyrimidine derivatives useful as pharmaceutically active compounds, in particular 1-[5-tert-butyl-3-[(1-methyltetrazol-5-yl)methyl]triazolo[4,5-d]pyrimidin-7-yl]pyrrolidin-3-ol.
专利号:WO-2025087822-A1 优先权日:2023-10-23 标 题 :New process for the preparation of (3r)-fluoropyrrolidine hydrochloride 发明人:ENGL PASCAL STEPHAN; HILDBRAND STEFAN; MOESSNER CHRISTIAN; STOECKLI MARKUS; STUTZ ALFRED 权利人:HOFFMANN LA ROCHE; HOFFMANN LA ROCHE 摘要:The present invention relates to a new process for the preparation of (3R)-3-fluoropyrrolidine hydrochloride or an acceptable salts thereof via a N-Boc-(3S)-3-hydroxypyrrolidine intermediate. The process is suitable for the synthesis of N-Boc-(3S)-3- hydroxypyrrolidine at technical scale in high, not less than 99.85%-a/a optical purity and a purity of not less than 99.8%-a/a. The high quality N-Boc-(3S)-3-hydroxypyrrolidine can be converted to (3R)-3-fluoropyrrolidine hydrochloride exhibiting an optical purity of not less than 99.95%-a/a and a purity of not less than 99.5%-a/a thus making it a suitable intermediate for manufacturing of pharmaceutical active compounds.
专利号:US-6566525-B1 优先权日:1998-09-17 标 题:Preparation of N-substituted-hydroxycycloalkylamine derivatives 发明人:KIM SEONG JIN; KIM KEON IL; YANG KYOUNG YOUL 权利人:SAMSUNG FINE CHEMICALS CO LTD 摘要:A process for the preparation of N-substituted-hydroxycycloalkylamine derivatives, that are useful intermediates for the synthesis of various organic chemicals including pharmaceutical and agrochemical compounds, represented by formula (1), by reacting a 1,2-dihydroxalkyl alcohol, represented by the following formula (2), with a thionyl halide to produce an intermediate 1,2-cyclosulfinylalkyl halide represented by the following formula (3); and then cyclizing that intermediate with an amine compounds represented by the following formula (4).In the above structural formuli, * represents an asymmetric carbon atom; R1 is hydrogen or an amino-protecting group; m is an integer of 1-3; and X is halogen. The reactant compounds as well as the compounds made according to this invention have the following substitution pattern:n=1, R2=OH, R3=H and m=1; n=1, R2=H, R3=CH2OH and m=2;n=2, R2=OH, R3=H; and m=2; and n=2, R2=H, R3=CH2OH and m=3.
参考文献:10.1055/s-2005-923584 摘要:Tomkinson NC, Bridgeman E. A Simple Method for the Preparation of Di-, Tri- and Tetrasubstituted Non-Symmetrical Ureas. Synlett. 2006;(2):243–6. doi: 10.1055/s-2005-923584. 参考文献:10.1055/s-0037-1610714 摘要:Steven A. Micelle-Mediated Chemistry in Water for the Synthesis of Drug Candidates. Synthesis. 2019 May 21;51(13):2632–47. doi: 10.1055/s-0037-1610714. 参考文献:10.1055/a-1911-6793 摘要:Lewkowicz ES, Lafuente L, Maidana LG, Bisceglia JA, Iribarren AM. Organocatalytic Synthesis of Benzimidazole Derivatives. Synthesis. 2022 Sep 15;54(24):5471–8. doi: 10.1055/a-1911-6793.