CAS: 2462-31-9; H-Dl-Gly-Obzl.Hcl

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叔丁氧羰基氨基-乙酸苄酯置于盐酸,乙酸乙酯体系中,化学反应生成甘氨酸苄酯盐酸盐
参考文献:Vertebrate Collagenase Inhibitor. Ii. Tetrapeptidyl Hydroxamic Acids.
标题:Vertebrate Collagenase Inhibitor. Ii. Tetrapeptidyl Hydroxamic Acids.
摘要:为了开发一种有效且特异性强的胶原酶抑制剂,研究人员合成了一系列四肽羟胺酸,这基于之前关于三肽衍生物的研究结果(chem. Pharm. Bull.,38,1007-1011,1990).在合成的四肽衍生物系列中,R-Gly-Pro-Leu-Ala-Nhoh 和 R-Gly-Pro-D-Leu-D-Ala-Nhoh 被发现对脊椎动物胶原酶具有高度特异性和有效抑制作用,Ic50 约为10^-6M,其中 R 代表 Boc 或酰基.对其结构-活性关系的分析显示了胶原酶底物结合位点的几个特征:1)s1 亚位点形成一个浅的疏水口袋,虽然甘氨酸残基对应于天然胶原底物的亚位点;2)s2 亚位点形成一个体积较大的口袋,对疏水性的需求较低;3)s3 亚位点优先容纳脯氨酸残基;4)肽类胶原酶抑制剂的 P4-P1 亚位点与 S4-S1 亚位点的结合是形成其羟胺酸基团与酶催化位点的锌离子紧密结合所必需的.将一个对映体二肽单元 D-Leu-D-Ala 引入到 P2-P1 亚位点中,显示出与胶原酶扩展的 S4-S1 亚位点的结合能力增加,从而提供了耐蛋白酶的抑制剂.
Doi:10.1248/cpb.39.1489

专利信息

专利号:WO-2011091548-A1
优先权日:2010-01-27
标 题:Method for cucurbitine synthesis
发明人：CHANG XIAOWEI; KHOSHDEL EZAT; PENG WEIMIN; WANG JINFANG; YAO YINFANG
权利人:UNILEVER PLC; UNILEVER NV; UNILEVER HINDUSTAN; CHANG XIAOWEI; KHOSHDEL EZAT; PENG WEIMIN; WANG JINFANG; YAO YINFANG
摘要:A method for the synthesis of cucurbitine comprising the step of forming a pyrrolidine ring by a 1,3 dipolar cycloaddition reaction.

专利号:US-5710246-A
优先权日:1996-03-19
标题 :Process for intermediates for the synthesis of LHRH antagonists
发明人：FUNK KENNETH W; LUNDELL EDWIN O; MILLER ROBERT B; CHANG JANE L; KISHORE VIMAL; NAPIER JAMES J; STAEGER MICHAEL A
权利人:ABBOTT LAB
摘要:A method is provided for preparing decapeptide and undecapeptide derivatives of LHRH by solution phase peptide chemistry as well as intermediate peptides useful in the same method.

专利号:US-8101665-B2
优先权日:2007-12-17
标题 :Process for synthesis of tritiated and deuterated thiorphan and acetorphan
发明人：MASJEDIZADEH MOHAMMAND R; WU SHAO-YONG
权利人:MASJEDIZADEH MOHAMMAND R; WU SHAO-YONG; ROCHE PALO ALTO LLC
摘要:Methods for preparing tritium or deuterium labeled thiorphan comprising reacting a compound of formula j n nwherein m is from 1 to 5 and X is halo, with Z 2 wherein Z is tritium or deuterium, in the presence of a catalyst, to form a compound of formula kn n nwherein n is from 1 to 5, provided that n is less than or equal to m.

专利号:US-2009215986-A1
优先权日:2006-03-08
标题:Solution Synthesis of Peptide Cell Growth Stimulators
发明人：EPSTEIN DAVID; KRUSZYNSKI MARIAN F; MARSH CHRISTOPHER; SCHMIDT ALBERT
权利人:EPSTEIN DAVID; KRUSZYNSKI MARIAN F; MARSH CHRISTOPHER; SCHMIDT ALBERT
摘要:A solution phase synthetic method for preparing basic tripeptides of the formula Gly-Xaa-Gly-X which have in various biological properties such as stimulating protein production when used as additives in a bioreactor. The basic tripeptides of the invention may be produced on gram or kilogram scale.

专利号:US-5710247-A
优先权日:1996-03-19
标题:Process and intermediates for the synthesis of LHRH antagonists
发明人：FUNK KENNETH W; LUNDELL EDWIN O; MILLER ROBERT B; CHANG JANE L; KISHORE VIMAL; NAPIER JAMES J; STAEGER MICHAEL A
权利人:ABBOTT LAB
摘要:A method is provided for preparing decapeptide and undecapeptide derivatives of LHRH by solution phase peptide chemistry as well as intermediate peptides useful in the same method.

专利号:US-5134231-A
优先权日:1985-12-28
标题 :3(1-hydoxyethyl)azetidinone compounds and their production
发明人：SUNAGAWA MAKOTO; NOZAKI YOSHIHITO; SASAKI AKIRA; MATSUMURA HARUKI
权利人:SUMITOMO PHARMA
摘要:An amino acid compound of the formula: ##STR1## wherein R is a lower alkyl group, R 1 is a hydrogen atom or a protecting group for carboxyl, R 2 is a hydrogen atom, a protecting group for amino, an optionally substituted allyl group of the formula: ##STR2## (wherein R 3 and R 4 are each a hydrogen atom, a lower alkyl group or an aryl group), a beta-hydroxyethyl group in which the hydroxyl group is optionally protected, a formylmethyl group in which the formyl group is optionally protected, a carboxymethyl group in which the carboxyl group is protected or a 2-furylmethyl group and X is an optionally protected carboxyl group, a hydroxymethyl group in which the hydroxyl group is optionally protected or a substituted mercaptomethyl group of the formula: n n --CH.sub.2 SR.sub.5 n n (wherein R 5 is an aryl group or an ar(lower)alkyl group), which is a useful intermediate in the synthesis of 1-alkylcarbapenem compounds.