CAS: 62129-44-6; Boc-Phe(4-I)-Oh

相似化合物

14173-41-2 176199-35-2 205526-29-0

上下游产品

tert-butyl dicarbonatedi-tert-butyl dicarbonate 4-iodo-L-phenylalanine 1-bromomethyl-4-iodobenzene diethyl tert-butoxycarbonylaminomalonatemethyl {(S)-2-[(tert-butoxycarbonyl)amino]-3-(4-iodophenyl)propanoyl}-L-phenylalaninate -L-phenylalanyl>-L-tyrosine methyl ester3-hydroxy-O-methyl-N-4-iodo-N-(1,1-dimethylethoxy)carbonyl-L-phenylalanyl-L-tyrosine methyl ester (S)-2-tert-Butoxycarbonylamino-3-{4-[4-((S)-2-tert-butoxycarbonylamino-2-methoxycarbonyl-ethyl)-phenylsulfanyl]-phenyl}-propionic acid B°C-Phe(I)-Gaba-OTmse

4-碘苄基溴置于sodium Hydride,溶剂黄146体系中,用 正己烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 22.5H,反应生成 Boc-4-碘-L-苯丙氨酸
参考文献:通过基于结构的药物设计,确定二肽腈为组织蛋白酶b的有效抑制剂和选择性抑制剂.
标题:通过基于结构的药物设计,确定二肽腈为组织蛋白酶b的有效抑制剂和选择性抑制剂.
摘要:组织蛋白酶b是半胱氨酸蛋白酶的木瓜蛋白酶超家族的成员,并且已与包括关节炎和癌症在内的多种疾病的病理学有关.为了确定这种蛋白酶的有效可逆抑制剂,我们从先前报道的cbz-Phe-Nh-Ch(2)cn(19,Ic(50)= 62 Microm)开始检查了一系列二肽腈. .高分辨率x射线晶体学数据和分子模型被用来优化此模板的p(1),P(2)和p(3)取代基.组织蛋白酶b在其类别中是独特的,因为它在活性位点的s(2)'口袋中包含一个羧酸盐识别位点.通过束缚从碳α到腈的羧酸盐官能团来与酶的该区域相互作用,可以提高抑制剂的效力和选择性.
DOI:10.1021/jm010206Q

专利信息

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-5783577-A
优先权日:1995-09-15
标题 :Synthesis of quinazolinone libraries and derivatives thereof
发明人：HOUGHTEN RICHARD A; OSTRESH JOHN M
权利人:TREGA BIOSCIENCES INC
摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.

专利号:WO-9834113-A1
优先权日:1997-02-04
标题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein
发明人：OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; HOUGHTEN RICHARD A; BLONDELLE SYLVIE E; SCHONER CHRISTA C
权利人:TREGA BIOSCIENCES INC
摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.

专利号:US-6359144-B1
优先权日:1997-02-04
标 题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein
发明人：OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; BLONDELLE SYLVIE E; SCHONER CHRISTA C; HOUGHTEN RICHARD A
权利人:LION BIOSCIENCE AG
摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.

专利号:WO-9811438-A1
优先权日:1996-09-13
标题 :Synthesis of quinazolinone libraries and derivatives thereof

专利号:WO-2023184731-A1
优先权日:2022-03-30
标题:Preparation method for 4- 10 boric acid-l-phenylalanine intermediate
发明人：TAO LULU; ZHU YIFAN; FAN MINHUA; HONG CHAO; DING YUANCHUN; GUO WEIGE; LU CUIJUN; ZHOU SHENGJUN
权利人:HAINAN POLY PHARM CO LTD; Zhejiang puli pharmaceutical co ltd; ANHUI PULI PHARMACEUTICAL CO LTD
摘要:The present invention relates to the technical field of boron-containing drugs for boron neutron capture therapy, and specifically to a preparation method for a 4- 10 boric acid-L-phenylalanine intermediate. The preparation method uses a compound of a structure of formula iii as a starting material to react with a boronizing reagent and a Grignard reagent to prepare the intermediate, wherein the boronizing reagent has a structure of formula (a): R 1 and R 2 are each independently an alkyl group and can be identical or different; or R 1 and R 2 can be cyclized with the oxygen atoms to which they are attached and the boron atom to form a 5- or 6-membered ring; R is an amino protecting group; X is a halogen. The 4- 10 boric acid-L-phenylalanine prepared by the method needs no purification: the HPLC content is greater than 98%, and the total yield of the product is greater than 80%, which completely meet the modern fine chemical synthesis requirements. The method can achieve the industrial production of 4- 10 boric acid-L-phenylalanine.