CAS: 121808-62-6; (R)-3-((S)-5-Oxopyrrolidine-2-Carbonyl)Thiazolidine-4-Carboxylic Acid

相似化合物

162148-17-6 117241-40-4 162148-15-4

上下游产品

CAS号28990-85-4 L-焦谷氨酸五氯苯基酯 | CAS号34592-47-7 L-硫代脯氨酸 | CAS号98-79-3 L-焦谷氨酸

Ethyl-(R)-3-<(S)-(5-Oxo-2-Pyrrolidinyl)Carbonyl>-Thiazolidine-4-Carboxylate置于盐酸体系中,用 水 用作溶剂,化学反应 2.0H,以47.2 G的收率获得匹多莫德
参考文献:一种匹多莫德的工业化规模制备方法
标题:一种匹多莫德的工业化规模制备方法
摘要:本发明为一种匹多莫德的工业化规模制备方法,属于药物合成领域.本发明采用l‑半胱氨酸关环,酯化得到l‑噻唑烷‑羧酸酯;然后与l‑焦谷氨酸在缩合剂作用下进行缩合,然后进行酯水解后结晶得到符合药用标准的产品.本发明不分离中间体l‑噻唑烷‑羧酸酯盐酸盐,缩合反应过程中通过共沸方法除水,减少了中间体分离与干燥步骤.与其它制备方法比较,本发明方法通过工艺优化,减少了大规模生产时间,提高了收率,降低了生产成本.本发明方法实现了匹多莫德规模化生产的可操作性.

专利信息

专利号:WO-2023233371-A1
优先权日:2022-06-03
标 题:A continuous flow process for synthesis of organic azides
发明人：GNANAPRAKASAM BOOPATHY; PANDEY AKANKSHA M; MONDAL SHANKHAJIT
权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE
摘要:The present disclosure relates generally to the field of synthetic organic chemistry. More specifically, the disclosure is directed to a continuous flow process for synthesis of azides from alcohols and peroxides, wherein the process comprises azidation with trimethylsilyl azide and a catalyst Amberlyst-15. It is a non-hazardous, mild and controlled reaction giving good yields of azides. The azides can be further employed for synthesis of medicinally and industrially useful chemicals.

专利号:US-11548898-B2
优先权日:2017-07-06
标题 :Synthesis of halichondrins
发明人：KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI
权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD
摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).

专利号:US-6423871-B1
优先权日:1999-02-26
标题 :Efficient synthesis of secondary amines by selective alkylation of primary amines
发明人：JUNG KYUNG WOON
权利人:UNIV SOUTH FLORIDA
摘要:A method for selective mono-N-alkylation of primary amines to produce secondary amines that are substantially free of overalkylated tertiary amines and quaternary ammonium salts, under mild reaction conditions without the necessity of protecting groups. Compounds of the class of secondary amines are produced by reacting an alkyl halide with an alkyl amine in anhydrous solvent, preferably dimethyl sulfoxide or N,N-dimethylformamide, in the presence of 0.1 to 3 molar equivalents of a cesium base. Optionally, the extent and selectivity of mono-N-alkylation is enhanced by addition to the reaction mixture of a powdered molecular sieve material for removal of water produced by the reaction, and/or tetrabutylammonium iodide to promote halide exchange. The invention permits selective and efficient mono-N-alkylation of a wide variety of substrates at 23° C.; does not cause racemization when used with enantiomerically-pure chiral substrates such as L-α-aminoesters; and is applied to solid phase synthesis whereby either the alkyl amine or alkyl halide is immobilized. The method is additionally used to produce polyamines, such as N-(2-(2-aminoethylthio)ethyl)ethylenediamine in 73% yield.

专利号:US-2023357286-A1
优先权日:2020-07-24
标 题:Ketone synthesis and applications
发明人：KISHI YOSHITO; UMEHARA ATSUSHI
权利人:HARVARD COLLEGE
摘要:Provided are new nickel./zirconium-mediated coupling reactions useful in the synthesis of ketone-containing compounds, e.g., halichondrin natural products and related molecules. A feature of the present disclosure is the use of a nickel(I) catalyst in tandem with a nickel (II) catalyst in the Ni/Zr-mediated coupling reactions. Without wishing to be bound by any particular theory, the nickel (I) catalyst selectively activates the electrophilic coupling partner (i.e., the compound of Formula (A)), and the nickel(ll) catalyst selectively activates the nucleophilic coupling partner (i.e., a thioester of Formula (B)). This dual catalyst system leads to improved coupling efficiency and eliminates the need for a large excess of one of the coupling partners (i.e., a compound of Formula (A) or (B)).

专利号:WO-0050377-A1
优先权日:1999-02-26
标 题:Efficient synthesis of secondary amines by selective alkylation of primary amines
发明人：JUNG KYUNG WOON
权利人:UNIV SOUTH FLORIDA
摘要:A method for selective mono-N-alkylation of primary amines to produce secondary amines that are substantially free of overalkylated tertiary amines and quaternary ammonium salts, under mild reaction conditions without the necessity of protecting groups. Compounds of the class of secondary amines are produced by reacting an alkyl halide with an alkyl amine in anhydrous solvent, preferably dimethyl sulfoxide or N,N-dimethylformamide, in the presence of 0.1 to 3 molar equivalents of a cesium base. Optionally, the extent and selectivity of mono-N-alkylation is enhanced by addition to the reaction mixture of a powdered molecular sieve material for removal of water produced by the reaction, and/or tetrabutylammonium iodide to promote halide exchange. The invention permits selective and efficient mono-N-alkylation of a wide variety of substrates at 23 °C; does not cause racemization when used with enantiomerically-pure chiral substrates such as L-α-aminoesters; and is applied to solid phase synthesis whereby either the alkyl amine or alkyl halide is immobilized. The method is additionally used to produce polyamines, such as N-(2-(2-aminoethylthio)ethyl)ethylenediamine in 73 % yield.

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.