CAS: 99295-81-5; (R)-2-Amino-3-Cyclopentylpropanoic Acid

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环戊烷三氟硼酸钾,L-丝氨酸置于rhodamine B,î²-Subunit Pyridoxal 5'-Phosphate Enzyme,Tryptophan Synthase From Pyrococcus Furiosus,E104G Mutant体系中,用 Aq. Phosphate Buffer 作为反应溶剂,以36%的收率获得产物
参考文献:协同光氧化还原-吡哆醛自由基生物催化立体选择性氨基酸合成
标题:协同光氧化还原-吡哆醛自由基生物催化立体选择性氨基酸合成
摘要:开发生物化学和有机化学中未知的合成有用的酶反应是生物催化中的一个重要挑战.通过光氧化还原催化和吡哆醛5'-磷酸(plp)生物催化的协同合并,我们开发了一种吡哆醛自由基生物催化方法来制备有价值的非经典氨基酸,包括那些带有立体化学二联体或三联体的氨基酸,而无需保护基团.使用工程化 Plp 酶,可以通过生物催化剂控制的方式生产任一对映体产物.协同光氧化还原-吡哆醛自由基生物催化代表了一个强大的平台,通过它可以发现以前未知的催化反应并驯服用于不对称催化的自由基中间体.
DOI:10.1126/science.Adg2420

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.