"Magic methyl effect" in medicinal chemistry and methylation of (hetero)arenes (ACS-Sp 2018) - Jan 27, 2018 - Abstract #MEDI 153; Pres time: Mar 18, 2018; 07:00 PM; Location: Hall E, Ernest N. Morial Convention Center; "A Ni-catalyzed methylation was developed using iodomethane or deuterated iodomethane as methyl source. The reaction is applicable to a wide range of substrates and allows installation of a CD3 group under mild reaction conditions without deuterium scrambling to other carbon atoms With using the method, SD-560 (potentially new drug for idiopathic pulmonary fibrosis) was prepared in gram quantities in just two steps with greater than 69% overall yield, compared to the existing method which resulted in less than 5% overall yield after seven steps." Biosimilar • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Respiratory Diseases
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Lu Hu;Xuebin Liao;Xin Liu;Yahu Arthur Liu
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