环丙基腈置于cobalt Pivalate,1,1,3,3-四甲基二硅氧烷,异氰酸叔丁酯,盐酸体系中,用 乙醚 作为反应溶剂,化学反应 24.5H,以98%的收率获得产物环丙基甲胺.盐酸盐 参考文献:钴-异氰化物催化剂将腈的氢硅烷还原为伯胺 标题:钴-异氰化物催化剂将腈的氢硅烷还原为伯胺 摘要:通过将1,1,3,3-四甲基二硅氧烷(tmds)作为氢化硅烷和催化量的与异氰配体缔合的co(opiv)2(piv = Co T Bu)的组合,可以将腈还原为甲硅烷基化的伯胺.将所得的甲硅烷基化的胺进行酸水解或用酰氯处理,以高收率得到相应的伯胺或酰亚胺.铁-钴双催化剂体系也可以通过氢化硅烷将伯酰胺一锅合成伯胺. DOI:10.1021/acs.Orglett.8B03736
专利信息
专利号:US-4150032-A 优先权日:1978-01-18 标 题 :9-Oxobenzomorphan process and intermediates 发明人:KAVADIAS GERRY 权利人:BRISTOL MYERS CO 摘要:Improved processes for preparing 2'-alkoxy-2,5-di-substituted-9-oxo-6,7-benzomorphans from benz[e]indolines and synthesis of the benz[e]indoline intermediates are described. A representative example involves synthesis of 9b-allyl-8-methoxy-3-methyl-5,9b-dihydrobenz[e]indoline and bromination thereof to 9b-allyl-4-bromo-8-methoxy-2,4,5,9b-tetrahydro-1H-benz[e]indole methylbromide which is then hydrolyzed with a weak base such as ammonium bicarbonate to provide 5-allyl-2'-methoxy-2-methyl-9-oxo-6,7-benzomorphan.
专利号:US-4234731-A 优先权日:1979-01-05 标题:9-Oxobenzomorphan process 发明人:KAVADIAS GERRY 权利人:BRISTOL MYERS CO 摘要:Improved processes for preparing 2'-alkoxy-2,5-di-substituted-9-oxo-6,7-benzomorphans from benz[e]indolines and synthesis of the benz[e]indoline intermediates are described. A representative example involves synthesis of 9b-allyl-8-methoxy-3-methyl-5,9b-dihydrobenz[e]indoline and bromination thereof to 9b-allyl-4-bromo-8-methoxy-2,4,5,9b-tetrahydro-1H-benz[e]indole methylbromide which is then hydrolyzed with a weak base such as ammonium bicarbonate to provide 5-allyl-2'-methoxy-2-methyl-9-oxo-6,7-benzomorphan.
专利号:US-10233182-B2 优先权日:2014-04-04 标题 :Substituted spirocyclic inhibitors of autotaxin 发明人:BABISS LEE; CLARK MATTHEW; KEEFE ANTHONY D; MULVIHILL MARK J; NI HAIHONG; RENZETTI LOUIS; RUEBSAM FRANK; WANG CE; XIE ZHIFENG; ZHANG YING 权利人:X RX INC 摘要:The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
专利号:US-9308194-B2 优先权日:2013-11-28 标 题:Indanyloxyphenylcyclopropanecarboxylic acids 发明人:LINGARD IAIN; HAMPRECHT DIETER 权利人:BOEHRINGER INGELHEIM INT 摘要:A compound of formula I, n nwherein the groups R 1 , R 2 , R 3 , X, m, and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-6180791-B1 优先权日:1989-03-23 标 题 :Synthesis of 8-substituted xanthines
专利号:US-7968584-B2 优先权日:2005-06-15 标 题:Substituted arylpyrazoles 发明人:BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL 权利人:PFIZER; PFIZER PROD INC 摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
参考文献:10.1023/a:1014464505261 摘要:Petricoul O, Claret L, Barbolosi D, Iliadas A, Puozzo C. Information Tools for Exploratory Data Analysis in Population Pharmacokinetics. Journal of Pharmacokinetics and Pharmacodynamics. 2001 Dec;28(6):577–99. doi: 10.1023/a:1014464505261.