CAS: 17791-52-5; Boc-His-Oh

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109425-51-6 123333-71-1 135610-90-1

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L-histidine hydr°Chloride monohydrate 2-(tert-Butoxycarbonyloxyimino)-2-phenylacetonitrile (S)-2-tert-Butoxycarbonylamino-3-[1-(4-methoxy-2,3,6-trimethyl-benzenesulfonyl)-1H-imidazol-4-yl]-propionic acid; compound with dicyclohexyl-amine N,1'-bis[(1,1-dimethylethoxy)carbonyl]-L-histidineL-Glutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosylglycyl-L-leucyl-L-arginyl-L-prolylglycinamide B°C-His(p-methoxybenzenesulfonyl)-OH α-B°C-L-histidine trimethylsilyl esterNα-B°C-L-histidine trimethylsilyl ester α-(tert-butyloxy)carbonyl-Nim-triphenylmethyl-L-histidineNα-(tert-butyloxy)carbonyl-Nim-triphenylmethyl-L-histidine

N,N'-二叔丁氧羰基-L-组氨酸 以 乙酸乙酯 用作溶剂,化学反应 3.0H,以85.1%的收率获得n-Boc-L-组氨酸
参考文献:一种nα-叔丁氧羰基-L-组氨酸的合成方法
标题:一种nα-叔丁氧羰基-L-组氨酸的合成方法
摘要:本发明涉及一种nα‑叔丁氧羰基‑l‑组氨酸的合成方法,包括如下步骤:将固体l‑组氨酸溶于碳酸钠水溶液中,滴加液体二碳酸二叔丁酯,反应完成后过滤,滤液用有机溶剂洗涤除去未反应的二碳酸二叔丁酯;水相酸化反应液后,加入萃取剂乙酸乙酯萃取,静置分层,油相洗涤,干燥,过滤得含中间体nα‑叔丁氧羰基‑nim‑叔丁氧羰基‑l‑组氨酸的乙酸乙酯溶液;将含中间体nα‑叔丁氧羰基‑nim‑叔丁氧羰基‑l‑组氨酸的乙酸乙酯溶液,在50~100oc下搅拌反应,反应结束后,经后处理得产物nα‑叔丁氧羰基‑l‑组氨酸.本发明提供的提供的nα‑叔丁氧羰基‑l‑组氨酸的合成方法工艺简单,操作方便,产品纯度及收率高于现有技术,解决使用离子交换树脂纯化和除盐不彻底的技术问题,适宜于工业化生产.

专利信息

专利号:WO-2023012709-A1
优先权日:2021-08-05
标 题 :An improved process for fmoc synthesis of semaglutide
发明人：LOBO LESTER JOHN; CHANDRAKESAN MURALIDHARAN; DOSHI CHETAN; CHANADAK SHAILESH LALCHAND; YADAV NANDLAL GOPAL; MOHE NIKHIL UMESH; VISHWANATHAN KODANDARAMAN
权利人:USV PRIVATE LTD
摘要:The present invention relates to an improved process for the synthesis of glucagon-like-peptide-1 (GLP-1) and its analogs by using combination of solid and solution phase synthesis of Fmoc protected amino acids in a sequential manner, optionally incorporating Boc protected dipeptide for unnatural amino acid in the Sequence of GLP-1, cleaving GLP-1 sequence from the resin followed by purification; attaching side-chain to the desired amino acid in the solution phase to synthesize desired GLP-1 analog, purifying it to Semaglutide. Temperature gradient is applied during initial coupling of amino acids to facilitate completion of difficult coupling reactions.

专利号:US-3988307-A
优先权日:1974-09-06
标题 :Solid phase synthesis of peptides with carboxyl-terminal amides
发明人：GROSS ERHARD
权利人:US HEALTH
摘要:The method of utilizing α,β-unsaturated amino acids, acyl, and N-acyl derivatives as linking agents in the solid phase synthesis of peptides with the corresponding production of carboxyl terminal amides. Preferred unsaturated amino acids are dehydroalanine and dehydrobutyrine which are constituents in naturally occurring amides such as nisin and subtilin. The synthesis follows conventional lines of R. B. Merrifield et al including blocking of the amino nitrogen, with the exception that the release agent contains an amount of water equimolar to the reactant α,β-unsaturated amino acid.

专利号:US-2024067694-A1
优先权日:2021-01-04
标 题:Synthesis of teduglutide
发明人：GANGA RAMU VASANTHAKUMAR; PATIL NITIN; SUVARNA DEEPA SHANKAR
权利人:BIOCON LTD
摘要:The present invention provides for novel synthetic approach of solid phase synthesis of peptides with C-terminal Aspartic acid by anchoring the side chain carboxylic group of aspartic acid to the solid support to avoid the formation of various impurities and thus resulting in higher yield and ease the purification process. The present invention further provides the usage of free amino acids and reducing agents as antioxidants in the cleavage cocktail to negate the formation of oxidative impurities formed during the global cleavage and isolation of the peptide from solid support.

专利号:US-7138526-B1
优先权日:1999-06-15
标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
发明人：HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M
权利人:AVENTIS PHARMA INC
摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries

专利号:US-2019177392-A1
优先权日:2014-09-23
标 题 :Synthesis of glp-1 peptides
发明人：PENIAS NAVON SHARON; NAVEH SHIRLY; VASILEIOU ZOI; BARLOS KONSTANTINOS
权利人:NOVETIDE LTD
摘要:Disclosed are processes for the synthesis of GLP-1 peptides, such as liraglutide and semaglutide, and a process for purifying liraglutide.

专利号:US-4101721-A
优先权日:1976-12-09
标题 :Solid phase synthesis of protected peptides
发明人：RICH DANIEL H; GURWARA SWEET K
权利人:WISCONSIN ALUMNI RES FOUND
摘要:The invention is addressed to the preparation of 3-nitro-4-bromomethyl benzoic acid, as a new compound from which 3-nitro-4-bromomethyl benzoyl amide polystyrene resin can be prepared for solid synthesis of protected peptide acids and amides and separation thereof without cleavage of acid labile protecting groups or decomposition of aromatic acid groups and from which purified polypeptides can be formed.