CAS: 167479-78-9; H-Phe(4-Cn)-Oh

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CAS号146664-08-6 2-乙酰氨基-3-(4-氰基苯基)-丙酸 | CAS号17201-43-3 α-溴对甲基苯甲腈 | CAS号104-85-8 对甲苯腈 | CAS号131724-45-3 B°C-L-4-氰基苯丙氨酸 | CAS号173963-93-4 FM°C-L-4-氰基苯丙氨酸

对氰基溴化苄置于盐酸,Lithium Hydroxide,Sodium Hydroxide,Sodium Ethanolate体系中,化学反应 77.25H,反应生成L-4-氰基苯丙氨酸
参考文献:使用tech 99M标记的高效gpiib / Iiia受体拮抗剂进行血栓成像.化学和初步生物学研究.
标题:使用tech 99M标记的高效gpiib / Iiia受体拮抗剂进行血栓成像.化学和初步生物学研究.
摘要:用发射伽马射线的放射性核素进行放射性标记的血小板特异性化合物可能特别适用于血栓的体内无创检测.描述了肽的合成,所述肽是血小板聚集的有效抑制剂,并且包含放射性核素-99M的螯合剂.设计目标化合物的目的是,可以在金属配位位置明确的位置制备稳定的氧v(v)物种.采用了一种策略,其中药效基团-Arg-Gly-Asp-(rgd)或rgd模拟物被限制在一个环中,该环是通过半胱氨酸残基与n端氯乙酰基的s-烷基化而形成的.通过用精氨酸模拟物s-(3-氨基丙基)半胱氨酸和4-Ami基苯基丙氨酸替代精氨酸来增强结合亲和力.通过合成包含两个或更多个含有受体结合区的环的低聚物,可以获得进一步的增强.看到的结合亲和力的增加超过了药效团的简单化学计量增加的预期.所描述的最有效的化合物具有约0.03 Microm的ic50,可抑制人的血小板凝集.用tech 99M标记两个更有效的肽(p280和p748),并在犬血栓形成模型中进行评估.这项工作中制备的99M
Doi:10.1021/jm950112E

专利信息

专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

专利号:US-9938509-B2
优先权日:2010-12-08
标 题 :Biocatalysts and methods for the synthesis of armodafinil
发明人：ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN
权利人:CODEXIS INC
摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.

专利号:US-5665598-A
优先权日:1994-04-13
标题:Synthesis of chiral N-protected-α-substituted-glycine free acids by zinc-mediated addition of organic halide to glycine cation equivalent
发明人：ABOOD NORMAN A; NOSAL ROGER A
权利人:SEARLE & CO
摘要:A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with alpha -chymotrypsin provides N-Boc-L-propargylglycine in high yield.

专利号:US-10087221-B2
优先权日:2013-03-21
标题 :Synthesis of hydantoin containing peptide products
发明人：HENKEL BERND
权利人:SANOFI AVENTIS DEUTSCHLAND
摘要:The present invention relates to a method of synthesizing a peptide product comprising at least one hydantoin group. The peptide product may be used as a reference material for the quality control of pharmaceutical peptides, particularly for the quality control of exendin peptides. Further, the invention relates to hydantoin building blocks, a method for manufacturing such building blocks and their use for the synthesis of peptide products.

专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.