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Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-01-13 , DOI: 10.1016/j.bmcl.2020.126963
Yusuke Sasaki 1 , Hidekazu Tokuhara 1 , Yusuke Ohba 1 , Atsutoshi Okabe 1 , Masaharu Nakayama 1 , Hideyuki Nakagawa 1 , Robert Skene 2 , Isaac Hoffman 2 , Hua Zou 2 , Masato Yoshida 1
Affiliation  

Herein we report an efficient method for the synthesis of a highly functionalized 2-pyrrolidinone, tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylate, from readily available starting materials. Utility of this compound was demonstrated in the synthesis of a novel series of macrocyclic Tyk2 inhibitors, leading to the identification of a potent and selective macrocyclic Tyk2 inhibitor (26).

中文翻译:

3-氰基-3-环丙基-2-氧吡咯烷-4-羧酸叔丁基酯的高效合成:高度官能化的2-吡咯烷酮,可使用新型大环Tyk2抑制剂。

在这里,我们报道了一种有效的方法,用于从容易获得的起始原料合成高度官能化的2-吡咯烷酮,3-氰基-3-环丙基-2-氧吡咯烷-4-羧酸叔丁酯。在合成一系列新的大环Tyk2抑制剂中证明了该化合物的效用,从而鉴定了一种有效的选择性大环Tyk2抑制剂(26)。
更新日期:2020-01-13
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