CAS: 16652-71-4; H-Pro-Obzl.Hcl

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苯甲醇置于盐酸,4-二甲氨基吡啶,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺体系中,用 1,4-二氧六环,二氯甲烷 用作溶剂,化学反应 23.0H,反应生成L-脯氨酸苄酯盐酸盐
参考文献:新的二价喹唑啉类似物作为iap拮抗剂的设计,合成和生物学评估
标题:新的二价喹唑啉类似物作为iap拮抗剂的设计,合成和生物学评估
摘要:我们最近报道了具有非常好效力的单价iap拮抗剂7的生物学评估(mda-Mb-231,Ic 50 = 19 Nm).为了提高细胞活性并改善类似药物的有利性质,我们基于7的喹唑啉结构新设计并合成了二价类似物.细胞效价和cyp抑制的优化导致27的鉴定,显示出超过100倍的急剧增加(ic 50 = 0.14 Nm),并在mda-Mb-231异种移植模型中引起实质性的肿瘤消退.这些结果强烈支持27作为一种有前途的二价拮抗剂,用于开发有效的抗肿瘤方法.
Doi:10.1016/j.Bmcl.2020.127676

专利信息

专利号:EP-0790982-B1
优先权日:1994-06-17
标 题 :Methods of synthesis of peptidyl argininals
发明人：WEBB THOMAS R; REINER JOHN E; TAMURA SUSAN Y; RIPKA WILLIAM C; DAGNINO RAYMOND JR; NUTT RUTH F
权利人:CORVAS INT INC
摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein, which have formula (I), wherein R1 is selected from the group consisting of hydrogen, benzyloxycarbonyl, isonicotinyloxycarbonyl, 2-chlorobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, t-butoxycarbonyl, t-amyloxycarbonyl, isobornyloxycarbonyl, adamantyloxycarbonyl, 2-(4-biphenyl)-2-propyloxycarbonyl, 9-fluorenylmethoxycarbonyl and methylsulfonylethoxycarbonyl; R2 is selected from the group consisting of alkyl of 1 to about 12 carbon atoms and aralkyl of about 7 to about 15 carbon atoms, either of which is optionally substituted with hydroxy or -CO-Y, wherein Y is hydroxy, alkoxy of 1 to about 12 carbon atoms, aralkoxy of about 7 to about 15 carbon atoms, O-polymeric support or NH-polymeric support; R3 is selected from the group consisting of hydrogen, Fmoc, nitro, benzyloxycarbonyl, t-butoxycarbonyl and adamantyloxycarbonyl; and R4 is selected from the group consisting of hydrogen, alkyl of 1 to about 12 carbon atoms, aryl of about 6 to about 14 carbon atoms and aralkyl of about 7 to about 15 carbon atoms; and salts thereof.

专利号:US-5731413-A
优先权日:1994-06-17
标 题:Method of synthesis of peptidyl aldehydes
发明人：WEBB THOMAS ROY; REINER JOHN EUGENE; TAMURA SUSAN YOSHIKO; RIPKA WILLIAM CHARLES; DAGNINO JR RAYMOND; NUTT RUTH FOELSCHE
权利人:CORVAS INT INC
摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel! reagents useful therein.

专利号:US-4801721-A
优先权日:1984-08-16
标题 :Stereospecific synthesis of carboxyalkyl peptides
发明人：RYAN JAMES W; CHUNG ALFRED
权利人:RYAN JAMES W; CHUNG ALFRED
摘要:Methods for the alkylation of substituted amines with trifluorate esters is disclosed.

专利号:US-7951834-B2
优先权日:2005-05-27
标题 :Angiotensin I-converting enzyme (ACE) inhibitors
发明人：STURROCK EDWARD; NCHINDA ALOYSIUS; CHIBALE KELLY
权利人:UNIV CAPE TOWN
摘要:This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACEâ€?, compound 5 a ) and analogues thereof. The synthesis process proceeds via an α,β-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.

专利号:WO-9535280-A1
优先权日:1994-06-17
标 题:Methods of synthesis of peptidyl argininals

专利号:US-6008367-A
优先权日:1996-06-25
标题:Intermediate for synthesis of anticoagulant agents