酶促化学合成及 3-氮杂双环[3.2.0]庚烷衍生物作为多巴胺能配体的评价。
Chemoenzymatic synthesis and evaluation of 3-azabicyclo[3.2.0]heptane derivatives as dopaminergic ligands.
机构信息
Institute of Chemistry, University of Tartu, Ravila 14, 50411 Tartu, Estonia.
出版信息
Eur J Med Chem. 2012 Sep;55:255-61. doi: 10.1016/j.ejmech.2012.07.025. Epub 2012 Jul 24.
PMID:22846798
Abstract
New 3-azabicyclo[3.2.0]heptane derivatives were synthesized using a multicomponent reaction. Racemic compounds were efficiently resolved by kinetic resolution with immobilized lipase B of Candida antarctica (Novozym 435). The obtained compounds demonstrated greater binding affinity at D(2L) and D(3) dopamine receptors compared to D(1) binding sites, and individual enantiomers of the same compound possessed distinct affinities.
摘要
新的 3-氮杂双环[3.2.0]庚烷衍生物是通过多组分反应合成的。使用固定化南极假丝酵母脂肪酶 B（诺维信 435）进行动力学拆分，可以有效地拆分外消旋化合物。与 D(1)结合位点相比，获得的化合物在 D(2L)和 D(3)多巴胺受体上表现出更高的结合亲和力，并且同一化合物的单个对映异构体具有不同的亲和力。
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