CAS: 42856-71-3; (S)-2-Methylpyrrolidine-2-Carboxylic Acid

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1508261-86-6 123053-48-5 63399-77-9

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CAS号132235-43-9 (S)-2-甲基吡咯烷-2-甲酰胺 | CAS号848488-83-5 H-DL-(αMe)Pro-NH2 | CAS号86046-11-9 (2R,5S)-2-tert-... | CAS号6931-10-8 5-methyl-1-oxid... | CAS号63399-71-3 1-[(Benzyloxy)c... | CAS号1031890-09-1 benzyl (S)-2-ca... | CAS号63399-73-5 (S)-2-甲基-2-吡咯烷羧酸 | CAS号132235-36-0 (1'R,2S,2'S,5'R... | CAS号1268519-85-2 (2S)-1,2-二甲基吡咯烷-2-羧酸 | CAS号109837-32-3 2-甲基-L-脯氨酸甲酯 (9ci) | CAS号103336-06-7 N-B°C-2-甲基-L-脯氨酸 | CAS号869001-86-5 (S)-1-(((苄氧基)羰基... | CAS号63399-71-3 1-[(Benzyloxy)c...

5-羟基-2-甲基-L-正缬氨酸置于氯化亚砜,Sodium Carbonate,三乙胺体系中,用 水,乙酸乙酯,异丙醇,乙腈 作为反应溶剂,化学反应 14.0H,反应生成 (S)-2-甲基脯氨酸
参考文献:一种光学活性2-甲基脯氨酸的制备方法
标题:一种光学活性2-甲基脯氨酸的制备方法
摘要:本发明公开了一种光学活性2‑甲基脯氨酸的制备方法.本发明以5‑羟基‑2‑戊酮(式1)为起始原料,先与氰化试剂缩合然后水解得到2‑氨基‑5‑羟基‑2‑甲基戊酸(式2),2‑氨基‑5‑羟基‑2‑甲基戊酸(式2)与拆分剂成盐析出进一步调ph析出光学活性的2‑氨基‑5‑羟基‑2‑甲基戊酸(式4);式4经氨基保护剂保护后得到式5,式5经氯化试剂氯化同时脱掉氨基保护基团得到式6化合物,然后一锅法环合得到光学活性2‑甲基脯氨酸(式7).该制备方法的综合收率高,成本低,反应条件温和,易于放大生产.

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:US-7820858-B2
优先权日:2006-03-25
标 题 :Concise β2-amino acid synthesis via organocatalytic aminomethylation
发明人：CHI YONGGUI; GELLMAN SAMUEL H; POMERANTZ WILLIAM C; HORNE WILLIAM S; GUO LI; ENGLISH EMILY P
权利人:WISCONSIN ALUMNI RES FOUND
摘要:The present invention provides a method for the synthesis of β 2 -amino acids. The method also provides methods yielding α-substituted β-amino aldehydes and β-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of β 2 -amino acids.

专利号:WO-2008098280-A1
优先权日:2007-02-16
标题:Methods for the synthesis of dicarba bridges in growth hormone peptides
发明人：ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA
权利人:POLYCHIP PHARMACEUTICALS PTY; UNIV MONASH; ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA
摘要:The invention relates to peptides comprising the carboxy terminal sequence of a growth hormone or an analogue of such a peptide in which the disulfide bridge is replaced by a dicarba bridge. Compositions containing such dicarba bridged peptides and method of treating obesity in an animal such as a human comprising administration of such dicarba bridged peptides are also disclosed.

专利号:US-2012095211-A1
优先权日:2010-09-22
标 题 :Substituted proline inhibitors of hepatitis c virus replication
发明人：BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D
权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC
摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.

专利号:US-2023364251-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人：BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

专利号:KR-20230118799-A
优先权日:2020-08-06
标题 :Chemical Synthesis of Large Enantiomer Proteins and Uses Thereof