CAS: 189337-28-8; (2R,3R)-2-(Fmoc-Amino)-3-Tert-Butoxy-1-Butanol

上下游产品

CAS号71989-35-0 Fm°C-Thr(tBu)-OH

N-[(苄氧基)羰基]-O-(2-甲基-2-丙基)-L-苏氨酸甲酯置于n-甲基吗啉,Sodium Tetrahydroborate,5%-Palladium/activated Carbon,氢气,氯甲酸乙酯,Sodium Carbonate,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,水,丙酮 用作溶剂,化学反应生成(2R,3R)-2-(Fmoc-氨基)-3-叔丁氧基-1-丁醇
参考文献:一种fmoc-O-叔丁基-L-苏氨醇的合成方法
标题:一种fmoc-O-叔丁基-L-苏氨醇的合成方法
摘要:本发明涉及一种fmoc‑o‑叔丁基‑l‑苏氨醇的合成方法.主要解决fmoc‑thr(Tbu)‑oh在硼氢化钠还原过程中,反应温度要求严格,且fmoc保护基团已分解,从而导致产率低,成本高的技术问题.本发明的合成方法包括以下步骤:A.L‑苏氨酸与氯化亚砜反应得到l‑苏氨酸甲酯盐酸盐;B.L‑苏氨酸甲酯盐酸盐在氢氧化钠作用下与氯甲酸苄酯反应得到z‑thr‑ome;C.Z‑thr‑ome在二氯甲烷,浓硫酸存在下,通入异丁烯反应,处理得到z‑thr(Tbu)‑ome;D.Z‑thr(Tbu)‑ome在丙酮和水存在的情况下,加入碱,皂化得到z‑thr(Tbu)‑oh;E.Z‑thr(Tbu)‑oh在四氢呋喃中,用硼氢化钠还原得到z‑thr(Tbu)‑ol;F.Z‑thr(Tbu)‑ol在甲醇中氢化得到h‑thr(Tbu)‑ol;G.H‑thr(Tbu)‑ol加入芴甲氧羰酰琥珀酰亚胺得到fmoc‑o‑叔丁基‑l‑苏氨醇.

专利信息

专利号:WO-2005087794-A1
优先权日:2004-03-12
标题:Process for octreotide synthesis
发明人：IAROV ALEXEI; AVRUTOV ILYA; LAZAROWYCH NATALIE; HOULDSWORTH STEPHEN
权利人:DALTON CHEMICAL LAB INC; IAROV ALEXEI; AVRUTOV ILYA; LAZAROWYCH NATALIE; HOULDSWORTH STEPHEN
摘要:A hybrid solid phase-liquid phase method of octreotide synthesis is described, along with methods for preparation of intermediate compounds useful in the synthesis of Octreotide. The method comprises liquid phase condensation of two or three peptide blocks, of which at least one is synthesized by solid-phase method. Each block contains two or more amino acid residues. The method combines the time and labor effectiveness of the solid-phase method with relative cheapness and easiness of purification of the product, characteristic of the liquid-phase method.

专利号:US-9388212-B2
优先权日:2013-02-21
标 题:Solid phase peptide synthesis via side chain attachment
发明人：BARLOS KLEOMENIS K
权利人:CHEMICAL & BIOPHARMACEUTICAL LAB OF PATRAS S A
摘要:The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.

专利号:US-7153933-B2
优先权日:2001-12-07
标 题 :Solid phase method for synthesis peptide-spacer-lipid conjugates, conjugates synthesized thereby and targeted liposomes containing the same
发明人：WU SHIH-KWANG; CHANG TING-GUNG; TSENG CHIN-LU; CHEN LI-JUNG; SHIH KAE-SHYANG
权利人:DEV CENTER BIOTECHNOLOGY
摘要:A solid phase synthesis method for preparing peptide-spacer-lipid conjugates, the peptide-spacer-lipid conjugates synthesized by the method, and liposomes containing the peptide-spacer-lipid conjugates. The present invention provides a convenient solid phase synthesis method for preparing peptide-spacer-lipid conjugates and provides various linkage groups (such as amide group) for conjugating peptide, spacer and lipid, wherein the spacer may comprise PEG. Several advantages can be achieved, such as the synthetic procedure can be simplified, the synthesis process can be set to automation, the purification is easier in each reaction step, and the product losses can be reduced to minimal during synthesis. The present synthesis method is suitable for preparing a wide range of peptide-spacer-lipid conjugates, provides a peptide-spacer-lipid conjugate prepared by the solid phase synthesis method of the present invention, which can be incorporated into a liposome as the targeting moiety for liposomal drug delivery to specific cells, and provides a targeting liposome containing the present peptide-spacer-lipid conjugate.

专利号:US-2004039161-A1
优先权日:2002-08-22
标 题:Use of trichloroacetimidate linker for peptide synthesis
发明人：MAYER JOHN PHILIP; YAN LIANG ZENG
摘要:The present invention provides a solid phase peptide synthetic method for the preparation of C-terminal alchohols, wherein the improvement consists of using trichloroacetimidate as the linker.

专利号:JP-2004189617-A
优先权日:2002-12-06
标题 :Solid-phase method for synthesis of peptide/spacer/lipid conjugate, conjugate synthesized thereby, and objective liposome containing the conjugate

专利号:CN-1837232-A
优先权日:2005-03-21
标 题:Process for solid phase synthesis of octreotide