| 摘要 |
<p>Preparing a 2-amino pyridine derivative comprises reacting an open-chain nitrile precursor with a nitrogen containing compound in a cyclization reaction. Preparing a 2-amino pyridine derivative of formula (II) comprises reacting an open-chain nitrile precursor of formula (NC-CH(R 1>)-C(R f)(OR 2>)-CH=CH-OR 3>) (I) or (NC-CH(R 1>)-C(R f)(OR 2>)-CH 2-CH(OR 6>)-OR 3>) (III) with a nitrogen containing compound of formula (N(H)(R 4>)(R 5>)) (IV) in a cyclization reaction. R fC nH (2n+1-m)X m; m : 1 to 2n+1; X : F, Cl or Br; n : 1-8; R 1>1-8C alkyl, 6-14C aryl, 1-13C heteroaryl, COOR, CN, SO2R, SOR or PO(OR) 2(all optionally substituted) or H; R 2>H or protecting group for alcohols; R 3>, R 6>1-8C alkyl, 1-8C acyl, 6-14C aryl or R 3silyl (all optionally substituted); either R 4>, R 5>1-8C alkyl, 6-14C aryl, 1-13C heteroaryl, 1-8C acyl or CONR 2(all optionally substituted) or H; or R 4>R 5>optionally substituted 4-8C alkylene chain, where a CH 2group is replaced by NH or O; and R : 1-8C alkyl, 6-14C aryl or 1-13C heteroaryl. Provided that when m is greater than 1, x is identical or different. [Image].</p> |
