发明名称 High yield method for stereoselective acylation of tertiary alcohols
摘要 The present invention is directed to methods of forming esters of tertiary alcohols. The methods include reacting a compound containing a tertiary alcohol with an acyl heteroaromatic ion-based compound of the formula:whereinR1 is an aromatic or aliphatic acid residue;Y is O or S;Z is CR2 or N;X is selected from the group consisting ofwherein R2 and R3 are independently selected from the group consisting of H, C1-6 alkyls, C1-6 substituted alkyls, C1-6 heteroalkyls, C3-8 branched alkyls, C3-8 cycloalkyls, C1-6 substituted heteroalkyls, aryls, substituted aryls, C1-6 alkyl aralkyls, C1-6 heteroalkyl aralkyls, C3-8 branched alkyl aralkyls and C3-8 cycloalkyl aralkyls; and R2' is the same as R2 except that R2' is not H;in the presence of a lanthanideIII metal-based catalyst and a base. In preferred embodiments, a substantially pure optical isomer of a compound containing a tertiary alcohol is used and the resultant esters are of sufficient purity so that expensive and time consuming recrystallization or purification steps are avoided.
申请公布号 US6194580(B1) 申请公布日期 2001.02.27
申请号 US20000495581 申请日期 2000.02.04
申请人 ENZON, INC. 发明人 GREENWALD RICHARD B.;PENDRI ANNAPURNA;ZHAO HONG
分类号 C07D498/22;(IPC1-7):C07D491/14 主分类号 C07D498/22
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