从丝氨酸、苏氨酸、β-苏氨酸和半胱氨酸的四聚体衍生物中合成 3-取代的焦谷氨酸。
Synthetic Access to 3-Substituted Pyroglutamic Acids from Tetramate Derivatives of Serine, Threonine, -Threonine, and Cysteine.
机构信息
The Department of Chemistry, Chemistry Research Laboratory , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , U.K.
Oxford Antibiotic Group, The Oxford Science Park, Magdalen Centre , Oxford OX4 4GA , U.K.
出版信息
J Org Chem. 2019 Aug 16;84(16):10257-10279. doi: 10.1021/acs.joc.9b01432. Epub 2019 Jul 29.
A general route which provides direct access to pyroglutamates from tetramates, making use of Suzuki coupling on an enol mesylate, followed by reduction, is reported. This work permits direct scaffold hopping from tetramate to substituted pyroglutamates. Some compounds in the library showed modest antibacterial activity against Gram-positive bacteria.
本文报道了一种从四氢叶酸出发、经烯醇甲磺酸的铃木偶联反应、还原反应，可直接得到焦谷氨酸的一般路线。该方法可实现四氢叶酸到取代焦谷氨酸的直接结构拼接。库中的一些化合物对革兰氏阳性菌表现出适度的抗菌活性。
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