CAS: 314741-40-7; (S)-Tert-Butyl 3-(Hydroxymethyl)Piperazine-1-Carboxylate

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CAS号314741-39-4 (S)-1-N-B°C-3-哌嗪甲酸甲酯 | CAS号848482-93-9 (S)-1-B°C-3-甲酸哌嗪 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号126872-94-4 (S)-2-羟基甲基哌嗪 | CAS号958635-18-2 (S)-3-氧代四氢-1H-恶... | CAS号788799-69-9 (S)-1-N-b°C-4-N... | CAS号958635-19-3 (S)-1,4-二叔丁基 2-... | CAS号958635-12-6 1,4-Piperazined... | CAS号147650-70-2 (S)-哌嗪-2-羧酸

(8As)-四氢-3-氧代-3H-恶唑并[3,4-A]吡嗪-7(1H)-羧酸叔丁酯置于lithium Hydroxide体系中,用 乙醇,水 用作溶剂,化学反应 1.5H,以21 G的收率获得(S)-1-Boc-3-羟甲基哌嗪
参考文献:差异保护的2-(羟甲基)哌嗪的实用合成
标题:差异保护的2-(羟甲基)哌嗪的实用合成
摘要:从光学活性的和可商购获得的(2 S)-哌嗪-2-羧酸二盐酸盐开始,提出了三种不同保护的2-(羟甲基)哌嗪的有效且可扩展的合成.这些合成构件可用于制备生物活性化合物,并用作构建组合文库的化学支架.
Doi:10.1021/jo701465H

专利信息

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.