CAS: 4043-88-3; (S)-2,5-Dihydro-1H-Pyrrole-2-Carboxylic Acid

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📜Boc-3,4-脱氢-L-脯氨酸 反应生成 3,4-脱氢-L-脯氨酸
参考文献:Ryan,James W.;Chung,Alfred
标题:Ryan,James W.;Chung,Alfred

专利信息

专利号:US-2023391818-A1
优先权日:2020-11-05
标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人：NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.

专利号:WO-2023214577-A1
优先权日:2022-05-02
标 题 :Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人：KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO; NOMURA KENICHI
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:The present invention addresses the problem of a desired elongation reaction not progressing as a result of a 6-membered cyclic amidine skeleton structure and a diketopiperazine formed when removing an N-terminated protective group during peptide synthesis. The inventors have discovered that it is possible to solve said problem during peptide production by treating a peptide protected by an N-terminated amino group in a protective group having an Fmoc skeleton by using a base which has a pKa of 23 or higher in an acetonitrile of a conjugate acid in a specific solvent, and next, performing peptide chain elongation.

专利号:US-5892038-A
优先权日:1997-12-08
标 题 :Hydroxy-amino acid amides
发明人：DOLLE III ROLAND ELLWOOD; PATEL HITESH K
权利人:PHARMACOPEIA INC
摘要:Compounds of Formula I I are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.

专利号:US-5872262-A
优先权日:1996-11-05
标 题:Hydroxy-amino acid amides
发明人：DOLLE ROLAND ELLWOOD III; JOHNSON THEODORE O JR; TAO SHIWEI
权利人:PHARMACOPEIA INC
摘要:Compounds of Formula I I are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.