| 摘要 |
<p>NEW MATERIAL:A compound expressed by formula I (R is H or amino- protecting group) R<1> is H, alkyl or halogen; R<2> is H or alkyl; Q is straight-chain or branched alkylene; Y is N3, OR<3> or NR<4>R<5>; R<3>-R<5> are H, alkylacyl or alkoxycarbonyl; m is 1 or 2) and salts thereof. EXAMPLE:N-(tert-Butoxycarbonyl)-3-ethylaminomethyl-3-pyrroline. USE:An intermediate for side chains of antimicrobial agents, antibiotic substances, etc. PREPARATION:A compound expressed by formula II (Am<1> is amino-protecting group; R<6> is alkyl) is reduced to provide a compound expressed by formula III (Q is CH2), which is then reacted with methanesulfonyl chloride, thionyl chloride, etc., at about 0 deg.C to convert the OH into a reactive group, such as sulfonyloxy or halogen. The resultant compound is subsequently reacted with sodium azide, etc., for forming an azide or ammonia, etc., for amination at about 100 deg.C for 10min-5hr to provide the aimed substance.</p> |
