CAS: 2133-40-6; H-Pro-Ome.Hcl

上下游产品

CAS号5211-23-4 N-Z-L-脯氨酸甲酯 | CAS号67-56-1 甲醇 | CAS号147-85-3 脯氨酸 | CAS号59936-29-7 (S)-1-叔-丁基-2-甲基... | CAS号2577-48-2 (S)-吡咯啉-2-羧酸甲酯 | CAS号74-88-4 碘甲烷 | CAS号175446-63-6 proline acid ch... | CAS号42429-27-6 L-脯氨酰胺盐酸盐 | CAS号59936-29-7 (S)-1-叔-丁基-2-甲基... | CAS号201406-78-2 methyl 1-benzyl... | CAS号147-85-3 脯氨酸 | CAS号23356-96-9 L-脯氨醇 | CAS号5211-23-4 N-Z-L-脯氨酸甲酯 | CAS号7531-52-4 L-脯氨酰胺 | CAS号73323-65-6 B°C-D-脯氨酸甲酯 | CAS号139419-63-9 METHYL(2S)-1-(1... | CAS号152668-35-4 L-Proline, 1-(2...

L-脯氨酸置于氯化亚砜体系中,用 甲醇 用作溶剂,以100%的收率获得l-脯氨酸甲酯盐酸盐
参考文献:卡托普利类似物作为金属β-内酰胺酶抑制剂
标题:卡托普利类似物作为金属β-内酰胺酶抑制剂
摘要:合成了许多卡托普利类似物,并作为金属β-内酰胺酶imp-1的抑制剂进行了测试.结构活性研究表明,甲基对于活性并不重要,并且可以通过缩短巯基烷酰基侧链的长度来最好地提高这些抑制剂的效力.用羧酸取代硫醇基导致活性完全丧失,而延长羧酸根基团的长度导致效力降低.用脯氨酸环取代哌啶酸可以维持非常好的活性.
Doi:10.1016/j.Bmcl.2016.02.007

专利信息

专利号:US-5554725-A
优先权日:1994-09-14
标题:Synthesis of dolastatin 15
发明人：PETTIT GEORGE R
权利人:UNIV ARIZONA
摘要:The present invention relates to the synthesis of natural (-)- dolastatin and the elucidation of the absolute configuration of this important sea hare constituent. A segment synthetic strategy was utilized for obtaining the Dolabella auricularia (Indian Ocean sea hare) depsipeptide dolastatin 15. Reaction of protected (S)-Hiva-(S)-Phe (2c) with isopropenyl chloroformate followed by Meldrum's ester, cyclization (2c→3a) of the product in toluene and finally methylation afforded the key (S)-dolapyrrolidine (Dpy) derivative (3b). Condensation of tripeptide (8) with the three unit Dpy segment (5b) followed by deprotection and coupling (diethyl phosphorocyanidate) led to dolastatin 15 in 11% overall yield. The powerful and selective activity of dolastatin 15 against the U.S. National Cancer Institute's panel of human cell lines is reported.

专利号:US-6887887-B2
优先权日:2001-03-19
标 题:Asymmetric synthesis of (S,S,R)-(-)-actinonin and its analogs and uses therefor
发明人：BORNMANN WILLIAM G; SIROTNAK FRANCIS; SCHER HOWARD; VIDAL EPHRAIM; BORELLA CHRISTOPHER; SCHEINBERG DAVID
权利人:SLOAN KETTERING INST CANCER
摘要:The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: n n nwhere R 1 is an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine, said R 1 further comprising a cyclic or bicyclic structure; R 2 is methyl, CH 2 CH 3 , (CH 2 ) 2 CH 3 , C(CH 3 ) 3 , phenyl, 3,4-dichlorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH 2 -(N-Boc-4-piperidine), 4-tetrahydropyran, CH 2 -4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl; R 3 is R 2 or C 3-8 alkyl, R 4 is C 1-3 alkyl; and R 5 is NH 2 , OH, NHOH, NHOCH 3 , N(CH 3 )OH, N(CH 3 )OCH 3 , NHCH 2 CH 3 , NH(CH 2 CH 3 ), NHCH 2 (2,4-(OCH3) 2 Ph, NHCH 2 (4-NO 2 )Ph, NHN(CH 3 ) 2 , proline, or 2-hydroxymethyl pyrrolidine. Additionally, a method for the treatment of a neoplastic disease or for the inhibition of tumor cell growth each comprising the step of administering to an individual in need of such treatment a pharmacologically effective dose of the compounds of the present invention are provided.

专利号:US-5468876-A
优先权日:1986-05-22
标题:Intermediates for the stereoconservative synthesis of 1-substituted (S)-and (R)-2-aminomethylpyrrolidines
发明人：FEDERSEL HANS-JUEGEN; HOE THOMAS; RAEMSBY STEN I; STROEM PETER H E
权利人:ASTRA AB
摘要:Disclosed are (R)- and (S)-isomers of the compounds of the Formulas II and III with at least 95% optical purity ##STR1## wherein R 1 and R 2 are the same or different and represent a hydrogen atom, a lower alkyl, lower alkenyl or lower alkynyl group, a cycloalkyl group or a group (CH 2 ) m Ph, wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group. n These compounds are intermediates in the stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines.

专利号:US-5076973-A
优先权日:1988-10-24
标题:Synthesis of dolastatin 3
发明人：PETTIT GEORGE R; HOLZAPFEL CEDRIC W
权利人:UNIV ARIZONA
摘要:Synthesis of dolastatin 3 is accomplished by one amino acid unit addition from L-Pro-OMe employing diethyl phosphorocyanidate-triethylamine for peptide bond formation and N-Boc protection (trifluoroacetic acid cleavage). Thereafter Boc-L-Leu-L-(gln)Thz-(gly)Thz-L-Val-L-Pro-OMe was obtained, successively crystallized from ethanol-diethyl ether, converted to the OPfp active ester, Boc cleavage and cyclization in dioxane containing t-butanol and 4-pyrrolidinopyridine to yield synthetic (-)-dolastatin 3.

专利号:US-2009099061-A1
优先权日:2006-01-27
标 题:Synthesis of carotenoid analogs or derivatives with improved antioxidant characteristics
发明人：FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F
权利人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F
摘要:A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.

专利号:US-7285667-B2
优先权日:2005-04-26
标题 :Process for the synthesis of functionalized indolizidines
发明人：GOPALSAMY ARIAMALA; SHI MENGXIAO
权利人:WYETH CORP
摘要:The present invention provides a process for the preparation of functionalized indolizidines comprising the steps and products disclosed within this application.