CAS: 7531-52-4; H-Pro-Nh2

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L-脯氨酸置于palladium On Activated Charcoal Sodium Hydroxide,氨,氢气,三乙胺,氯甲酸异丁酯体系中,用 甲醇,水 作为反应溶剂,化学反应 11.0H,反应生成 L-脯氨酰胺
参考文献:2-氨基甲基吡咯烷(1,1-环丁烷-二羧酸基)铂(II)旋光异构体的合成,抗肿瘤活性和肾毒性
标题:2-氨基甲基吡咯烷(1,1-环丁烷-二羧酸基)铂(II)旋光异构体的合成,抗肿瘤活性和肾毒性
摘要:合成了2-氨基甲基吡咯烷(1,1-环丁烷-二羧甲基)铂(II)(dwa2114,1)的旋光异构体,该异构体对各种肿瘤均具有有效的抗肿瘤活性.在sc-Iv系统中检查了它们对结肠26癌的抗肿瘤活性,并将药物治疗小鼠的尿蛋白和糖水平变化用作肾毒性指标.就其对肿瘤的影响而言,(+)-(S)-2-氨基甲基吡咯烷(1,1-环丁烷二羧基++ +)铂(II)(6B)比对映体6A更有效,因为有效剂量6B小于对映体6A.的6A; 但是,两种药物均显示出有效的抗肿瘤活性.另一方面,在6A和6B之间的肾毒性方面显示出明显的差异.异构体6B诱导小鼠尿蛋白和糖水平显着增加,
DOI:10.1002/jps.2600800907

专利信息

专利号:US-5468876-A
优先权日:1986-05-22
标题:Intermediates for the stereoconservative synthesis of 1-substituted (S)-and (R)-2-aminomethylpyrrolidines
发明人：FEDERSEL HANS-JUEGEN; HOE THOMAS; RAEMSBY STEN I; STROEM PETER H E
权利人:ASTRA AB
摘要:Disclosed are (R)- and (S)-isomers of the compounds of the Formulas II and III with at least 95% optical purity ##STR1## wherein R 1 and R 2 are the same or different and represent a hydrogen atom, a lower alkyl, lower alkenyl or lower alkynyl group, a cycloalkyl group or a group (CH 2 ) m Ph, wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group. n These compounds are intermediates in the stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines.

专利号:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人：CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

专利号:US-7951905-B2
优先权日:2006-09-18
标 题 :Synthesis of carbohydrate-templated amino acids and methods of using same
发明人：SCHWEIZER FRANK; ZHANG KAIDONG; OWENS NEIL; ZHANEL GEORGE
权利人:UNIV MANITOBA
摘要:The present invention generally relates to tetrahydropyranyl-derivatized amino acids, their syntheses and their incorporation into peptides and peptidomimetics. The tetrahydropyran moiety constrains the side chain of an amino acid, thereby providing a molecule that may act as a sugar- or amino acid-mimetic as well as a scaffold for combinatorial synthesis.

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:US-2022356182-A1
优先权日:2009-03-27
标题 :Inhibitors of hepatitis c virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-2023407293-A1
优先权日:2021-10-27
标 题:Dna-encoded and affinity-tagged masked-warhead compounds and use thereof in assembling libraries of small molecules enabled for late-stage purification and multiplexed screening of covalent ligands
发明人：MAIANTI JUAN PABLO
权利人:MAIANTI JUAN PABLO
摘要:The present disclosure relates to DNA-encoded and affinity-tagged masked warhead installation compounds and use thereof in the synthesis of electrophilic warhead DNA-Encoded Libraries (eDEL), including substituted and unsubstituted acrylamide warheads, which can be purified from unreacted library intermediates and byproducts.