Rapid parallel liquid-phase synthesis of pyrazoles has first been developed. The 1,3-dipolar cycloaddition be-tween nitrilimines generated in situ and soluble polymer-supported alkynyl or alkenyl dipolarophiles in par...Rapid parallel liquid-phase synthesis of pyrazoles has first been developed. The 1,3-dipolar cycloaddition be-tween nitrilimines generated in situ and soluble polymer-supported alkynyl or alkenyl dipolarophiles in parallel one-pot fashion gave the corresponding PEG-supported regioisomeric pyrazoles or regiospecific pyrazolines. The latter was assuredly oxidated by DDQ to PEG-supported regiospecific pyrazoles. Cleavage from the support under mild conditions afforded pyrazoles in good yields and high purity.展开更多
基金Project supported by the National Natural Science Foundation of China (No. 20272051) and the Teaching and Research Award Program for Out-standing Young Teachers in Higher Education Institutions of Ministry of Education China.
文摘Rapid parallel liquid-phase synthesis of pyrazoles has first been developed. The 1,3-dipolar cycloaddition be-tween nitrilimines generated in situ and soluble polymer-supported alkynyl or alkenyl dipolarophiles in parallel one-pot fashion gave the corresponding PEG-supported regioisomeric pyrazoles or regiospecific pyrazolines. The latter was assuredly oxidated by DDQ to PEG-supported regiospecific pyrazoles. Cleavage from the support under mild conditions afforded pyrazoles in good yields and high purity.