专利号:US-3875167-A 优先权日:1972-05-26 标 题 :Synthesis of thalicarpine 发明人:KUPCHAN S MORRIS; LIEPA ANDRIS J 权利人:RESEARCH CORP 摘要:There is disclosed a novel total synthesis of thalicarpine which includes inter alia a total synthesis of hernandaline. The novel process is characterised in utilizing simple and readily available starting materials to form a diaryl ether system which is then condensed with a 3,4-dihydroisoquinolinium salt which is then converted to hernandaline. Hernandaline is reacted with a bicyclic Reissert compound to yield a compound having the thalicarpine skeleton, nascent hydrogen reduction yields Nmonodesmethyl thalicarpine which is methylated.
专利号:US-6248891-B1 优先权日:1997-05-23 标题:Synthesis of acridine derivative multidrug-resistant inhibitors 发明人:SHARP MATTHEW JUDE; MADER CATHERINE J; STRACHAN CALUM 权利人:GLAXO WELLCOME INC 摘要:Synthesis of the MDRI of formula (I) from intermediates of acridone acid of formula (II) and aminophenethyl isoquinoline of formula (III), via steps including coupling and conversion to yield the MDRI of formula (I).
专利号:US-8506927-B2 优先权日:2011-01-05 标 题 :Pegylated fluorobenzamide analogues, their synthesis and use in diagnostic imaging 发明人:MACH ROBERT H; TU ZHUDE 权利人:MACH ROBERT H; TU ZHUDE; UNIV WASHINGTON 摘要:Pegylated fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labeled with a positron-emitting radioisotope such as 18 F, can be used as radiotracers for medical imaging such as imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labeled with 123 I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
专利号:US-7872138-B2 优先权日:2006-08-07 标 题 :Process for the preparation of substituted-1,2,3,4-tetrahydroisoquinoline derivatives 发明人:VILLANI FRANK J; ZHONG HUA 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to a process for the synthesis of substituted-1,2,3,4-tetrahydroisoquinoline derivatives, useful as intermediates in the synthesis of pharmaceutical agents.
专利号:US-9458111-B2 优先权日:2010-07-29 标题:Process for the synthesis of substituted urea compounds 发明人:LEARMONTH DAVID ALEXANDER; BROADBELT BRIAN; WAHNON JORGE BRUNO REIS 权利人:LEARMONTH DAVID ALEXANDER; BROADBELT BRIAN; WAHNON JORGE BRUNO REIS; BIAL—PORTELA & CA S A 摘要:A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof: n nthe process comprising the reaction of a carbamate of Formula (II′): Formula (I′):n n nwith a primary or secondary amine of the formula R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
专利号:US-2015197503-A1 优先权日:2012-07-27 标题 :Process for the synthesis of substituted urea compounds 发明人:RUSSO DOMENICO; WAHNON JORGE BRUNO REIS; MATON WILLIAM; ESZENYI TIBOR 权利人:BIAL PORTELA & Cª S A 摘要:A process for preparing a substituted urea compound of Formula II or Formula I, or a pharmaceutically acceptable salt or ester thereof, Formula II, Formula I the process comprising the reaction of an intermediate of Formula II′ or Formula 1′, Formula II′, Formula I′ with a carbamoyl halide of the formula: R1R2NC(=0)Hal, in a solvent consisting essentially of pyridine, wherein Hal represents Cl, F, I or Br, and wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.