CAS: 175453-08-4; Fmoc-Phe(4-Cl)-Oh

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14091-08-8 14173-39-8 142994-19-2

上下游产品

9-芴甲基-N-琥珀酰亚胺基碳酸酯 N-(9H-Fluoren-2-Ylmethoxycarbonyloxy)Succinimide 82911-69-1

Dl-4-氯苯丙氨酸置于甲酸,Palladium 10% On Activated Carbon,碳酸氢钠,Sodium Carbonate,Sodium Hydroxide体系中,用 1,4-二氧六环,甲醇,水,N,N-二甲基甲酰胺,丙酮 用作溶剂,化学反应 9.0H,反应生成N-芴甲氧羰基-L-4-氯苯丙氨酸
参考文献:含卤化氨基酸的 Bim-23052 新类似物的合成,体外生物活性,水解稳定性和对接
标题:含卤化氨基酸的 Bim-23052 新类似物的合成,体外生物活性,水解稳定性和对接
摘要:一种有效的生长抑素类似物,Bim-23052 (Dc-23-99) D-Phe-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-Nh 2,已在 Nm 浓度下建立了体外生长激素抑制活性.它还具有对一些生长抑素受体的高亲和力的特点,这些受体主要分布在许多肿瘤细胞的细胞膜中.在此,我们报告了使用标准固相肽法 Fmoc/otbu-Strategy 合成一系列含有卤化 Phe 残基的 Bim-23052 类似物.在体外针对两种人类肿瘤细胞系(乳腺癌细胞系和肝细胞癌细胞系)以及人类非致瘤性上皮细胞系测试了这些化合物的细胞毒性作用.含有氟苯丙氨酸的类似物在 μm 范围内具有细胞毒性,因为含有 Phe (2-F) 的类似物对人肝细胞癌细胞系显示出更好的选择性.所提出的研究还表明,根据测试的细胞系,卤化 Phe 残基的积累不会增加细胞毒性.计算出的选择性指数揭示了母体化合物 Bim-23052
Doi:10.1007/s00726-020-02915-3

专利信息

专利号:US-8828938-B2
优先权日:2009-04-24
标 题:Method for the manufacture of degarelix
发明人：ZHANG HAIXIANG; FOMSGAARD JENS; STAERKAER GUNNAR
权利人:POLYPEPTIDE LABORATORIES AS
摘要:In a step-wise synthesis of degarelix comprising 0.3% by weight or less of 4-([2-(5-hydantoyl)]acetylamino)-phenylalanine analog on (solid support)-NH 2 a step comprises providing a solution of an amino acid or peptide of which the α-amino group is protected by Fmoc; contacting the support with the solution in the presence of reagent for forming a peptide bond between a carboxyl group of the amino acid or peptide and (solid support)-NH 2 ; removing Fmoc by contacting the support with an organic base, in particular piperidine, in an organic solvent. Also disclosed is degarelix of high purity prepared by the method of the invention and the use of Fmoc in the synthesis of degarelix.

专利号:US-8598089-B2
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries
发明人：MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A
权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC
摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.

专利号:US-8410028-B2
优先权日:2003-12-17
标 题:Methods for synthesis of encoded libraries
发明人：MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A
权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC
摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.

专利号:US-2007042401-A1
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries

专利号:US-2012245040-A1
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries

专利号:US-2009062147-A1
优先权日:2003-12-17
标 题:Methods for synthesis of encoded libraries