📜丙腈置于[ru(H)(Bh4)(Co)(Pph3)(3-(Di-Tert-Butylphosphino)-N-((1-Methyl-1H-Imidazol-2 yl)Methyl)Propylamine)],氢气,盐酸体系中,用 异丙醇,甲醇 作为反应溶剂,化学反应 3.5H,以98%的收率获得产物盐酸丙胺 参考文献:Nnp型夹钳咪唑基膦钌配合物:在温和条件下有效地进行芳香族和脂肪族腈的无碱加氢 标题:Nnp型夹钳咪唑基膦钌配合物:在温和条件下有效地进行芳香族和脂肪族腈的无碱加氢 摘要:已合成并充分表征了一系列七个新型的n Im N H P型钳型咪唑基膦膦钌配合物.使用苯甲腈加氢作为基准测试,确定了[ruhcl(co)(n Im N H P T Bu)]是最具活性的催化剂.凭借其稳定的ru-Bh 4类似物(其中氯化物被bh 4替代),已在温和且无碱的条件下氢化了多种(杂)芳族和脂肪族腈,包括工业上有用的己二腈. DOI:10.1002/chem.201504709
专利号:US-2025188502-A1 优先权日:2022-03-10 标 题 :Biocatalyst and method for the synthesis of ubrogepant intermediates 发明人:CHEN HAIBIN; HU HU; CAI BAOQIN; XU JUNPENG; LIU SITONG; JIN LUPING; WU XINWEI; CUI QINYAN; ZHANG CHENGXIAO; ZHU KAILONG 权利人:ENZYMASTER NINGBO BIO ENG CO LTD 摘要:This application provides engineered transaminase polypeptides for the synthesis of Ubrogepant intermediates with high stereoselectivity, high catalytic activity and good stability. This application also provides a reaction process for the asymmetric synthesis of Ubrogepant intermediates using the transaminase polypeptide.
专利号:US-6133018-A 优先权日:1997-06-02 标 题 :Enzymatic synthesis of chiral amines using -2-amino propane as amine donor 发明人:WU WEI; BHATIA MOHIT B; LEWIS CRAIG M; LANG WEI; WANG ALICE L; MATCHAM GEORGE W 权利人:CELGRO 摘要:2-Aminopropane is used as the amine donor in the stereoselective synthesis of a chiral amine from a ketone with a transaminase. In a typical embodiment, (S)-1-methoxy-2-aminopropane is prepared by bringing methoxyacetone into contact with a transaminase in the presence of 2-aminopropane as an amine donor until a substantial amount of methoxyacetone is converted to (S)-1-methoxy-2-aminopropane and 2-aminopropane is converted to acetone. In a second embodiment, L-alanine is prepared by bringing pyruvic acid into contact with a transaminase in the presence of 2-aminopropane as an amine donor.
专利号:EP-1075534-B8 优先权日:1998-03-11 标 题 :Improvements in the enzymatic synthesis of chiral amines 发明人:WU WEI; BHATIA MOHIT B; LEWIS CRAIG M; LANG WEI; WANG ALICE; MATCHAM GEORGE W 权利人:CELGRO 摘要:2-Aminopropane is used as the amine donor in the stereoselective synthesis of a chiral amine from a ketone with a transaminase. In a typical embodiment, (S)-1-methoxy-2-aminopropane is prepared by bringing methoxyacetone into contact with a transaminase in the presence of 2-aminopropane as an amine donor until a substantial amount of methoxyacetone is converted to (S)-1-methoxy-2-aminopropane and 2-aminopropane is converted to acetone. In a second embodiment, L-alanine is prepared by bringing pyruvic acid into contact with a transaminase in the presence of 2-aminopropane as an amine donor.
专利号:WO-2013113319-A1 优先权日:2012-01-31 标题 :Process for the preparation of strontium ranelate, intermediate or hydrates thereof 发明人:KOFTIS THEOCHARIS V; ROHIT RAVIKANT SONI; BHARAT BECHARBHAI BODA; DIPAKKUMAR NARSIBHAI BHUT; VIMALKUMAR SUBHIRBHAI PATEL 权利人:PHARMATHEN SA; KOFTIS THEOCHARIS V; ROHIT RAVIKANT SONI; BHARAT BECHARBHAI BODA; DIPAKKUMAR NARSIBHAI BHUT; VIMALKUMAR SUBHIRBHAI PATEL 摘要:The present invention relates to an improved process for the synthesis of strontium ranelate compound of formula I or its hydrates thereof. More particularly, the present invention relates to an economically viable and industrially feasible process for the preparation of strontium ranelate, intermediate or its hydrates thereof.
专利号:US-10329268-B2 优先权日:2013-09-13 标 题 :Processes for preparing medicaments for the treatment of cardiovascular diseases and intermediates for use therein 发明人:RUSSO DOMENICO; WAHNON JORGE; MATON WILLIAM; WEBER BEAT T; JERONIMO PAULA; SOUSA LUISA; BARROCAS PEDRO; PIRES RITA; LIMA RICARDO; VASCONCELOS TEOFILO 权利人:BIAL PORTELA & CA SA 摘要:The present invention provides a compound of formula N wherein: X is CH 2 , oxygen or sulphur; R 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group, wherein N is in the form of the individual R- and S-enantiomer or a mixture of the (R)- and (S)-enantiomer. The present invention also provides a compound of formula MA. The present invention also provides processes for preparing the above compounds, and processes involving their use. The compounds are particularly useful as intermediates in the synthesis of peripherally-selective inhibitors of dopamine-β-hydroxylase.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
[参考文献]: F De Croo, Et Al. High-Performance Liquid Chromatographic Behaviour Of Some Pharmaceutically Important Thiazide, Loop And Potassium-Sparing Diuretics. J Chromatogr. 1985 Jun 7;325(2):395-411.
合成参考文献
摘要:Jończyk, A.; Kowalkowska, A., Science of Synthesis, (2006) 8, 1160.