Benzyl 4-(Tetrahydrofuran-2-Carbonyl)Piperazine-1-Carboxylate置于palladium On Activated Charcoal,氢气体系中,用 甲醇 作为反应溶剂,以97.4 %的收率获得产物四氢糠酰哌嗪 参考文献: Ras Inhibitors,Compositions And Methods Of Use Thereof[fr] Inhibiteurs De Ras,Compositions Et Procédés D'Utilisation De Ceux-Ci 标题: Ras Inhibitors,Compositions And Methods Of Use Thereof[fr] Inhibiteurs De Ras,Compositions Et Procédés D'Utilisation De Ceux-Ci 摘要:There Is Provided A Compound Of Formula (I),And Its Use For Inhibiting Ras (Wild Type Or Mutant),For Example Hras,Nras,And/or Kras,And For The Prevention Or Treatment Of A Disease Or Disorder Associated With Abnormal Ras Activity,For Example Abnormal Ras Activity Caused By A Mutation In Ras,Including Cancers With A Mutated Ras. (I)
专利号:US-6080860-A 优先权日:1992-08-31 标 题:Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor 发明人:KARIMIAN KHASHAYAR; MURTHY KESHAVA; HALL DARREN 权利人:BRANTFORD CHEMICALSS INC 摘要:Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.
专利号:US-2008039473-A1 优先权日:2006-08-08 标题:Preparation and utility of substituted quinazoline compounds with alpha-adrenergic blocking effects 发明人:GANT THOMAS G; SARSHAR SEPEHR 权利人:AUSPEX PHARMACEUTICALS INC 摘要:The present disclosure is directed to modulators of alpha-adrenergic receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of hypertension, cardiac failure, prostatitis, and benign prostatic hyperplasia, and any other condition in which it is beneficial to modulate an alpha-adrenergic receptor.
专利号:WO-9405628-A1 优先权日:1992-08-31 标 题 :Synthesis of 2-substituted quinazoline compounds (such as terazosin) and meobentine and bethanidine and intermediates therefor
专利号:EP-0656885-A1 优先权日:1992-08-31 标 题 :Synthesis of 2-substituted quinazoline compounds (such as terazosin) and meobentine and bethanidine and intermediates therefor
专利号:US-5508306-A 优先权日:1992-11-13 标题:Aromatic amine derivatives 发明人:CHIU GEORGE; GLUCHOWSKI CHARLES 权利人:SYNAPTIC PHARMA CORP 摘要:This invention relates to novel aromatic amine compounds having the structure: ##STR1## where each W, Z 1 and Z 2 is independently H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, OH, F, Cl, Br, I, NO 2 , CN, SO 2 NHR 3 , NR 4 2 , CONR 3 2 , COR 5 ; where each R 1 and R 2 is independently H, C 1 -C 6 straight or branched chain alkyl or phenyl; where each X and Y is independently CH 2 , NR 4 , S, Sâ•?O, SO 2 ; where n is 0, 1 or 2; where each p and q is independently 1 or 2; where R 3 is H, C 1 -C 6 straight or branched chain alkyl or phenyl; where R 4 is H, C 1 -C 6 straight or branched chain alkyl or COR 3 ; and where R 5 is H, C 1 -C 6 straight or branched chain alkyl or phenyl, C 1 -C 6 straight or branched chain alkoxy or OH. n In addition the invention includes using such compounds for the treatment of benign prostatic hyperplasia, lowering intraocular pressure and inhibiting cholesterol synthesis.