CAS: 663948-85-4; Tert-Butyl ((3S,5S)-5-(Hydroxymethyl)Pyrrolidin-3-yl)Carbamate

相似化合物

1264243-44-8 1265964-45-1 1217975-63-7

上下游产品

CAS号380648-94-2 (2S,4S)-苄基4-((叔... | CAS号64187-48-0 N-CBZ-羟脯氨酸甲酯 | CAS号113490-74-7 4(S)-azido-N-[(... | CAS号117811-78-6 (2S,4R)-Cbz-4-甲... | CAS号207304-86-7 (2S,4S)-1-CBZ-4... | CAS号168263-80-7 (2S,4S)-1-苄基 2-... | CAS号51-35-4 L-羟脯氨酸 | CAS号13504-85-3 CBZ-L-羟脯氨酸

📜(2S,4S)-1-Cbz-4-氨基吡咯烷-2-羧酸甲酯置于palladium On Activated Charcoal 锂硼氢,氢气,三乙胺体系中,用 四氢呋喃,甲醇,二甲基亚砜 作为反应溶剂,化学反应 18.5H,反应生成 [(3S,5S)-5-(羟甲基)-3-吡咯烷基]氨基甲酸叔丁酯
参考文献:吡咯烷氨基甲酸酯核酸:合成和dna结合研究.
标题:吡咯烷氨基甲酸酯核酸:合成和dna结合研究.
摘要:报道了吡咯烷氨基甲酸酯核酸的有效固相合成.被保护的(2S,4S)-4-氨基吡咯烷-2-甲醇的核苷胸腺嘧啶和胞嘧啶通过乙酰基连接到环氮上,可以活化为碳酸硝基苯酯,用于合成二聚体,三聚体和低聚物.
DOI:10.1016/s0968-0896(03)00331-6

专利信息

专利号:US-10017481-B2
优先权日:2012-03-17
标 题 :Conformationally constrained, fully synthetic macrocyclic compounds
发明人：OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC
权利人:POLYPHOR AG
摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

专利号:US-9695191-B2
优先权日:2009-08-05
标题 :Conformationally constrained, fully synthetic macrocyclic compounds
发明人：OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN
权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG
摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.