| 摘要 |
<p>Cpds. (I): (where R is H, 1-6C alkyl or Ar-A; Ar is phenyl opt. substd. by one or two halogen, CF3, 1-5C alkyl, 1-6C alkoxy, -OCH2O-, OH, or COOMe gps. or by one or more NO2, NH2, MeCONH, PhCONH, p-Cl-C6H4CONH-, o-HO-C6H4CONH, MeSO2NH, NH2SO2, Me2NSO2 or Et2NSO2 gps.; A is polymethylene of =6C or CH(Ph)(CH2)m (m is 0 or 1-4), -CH=CH-CH2-CH2CHOHCH2, O-CH2CH2 or CH(OMe)-, -NHCOCH2- or CO(CH2)p (p is 0 or 1-4) and R1 is H, alkyl or opt. substd. phenyl) are prepd. by reacting (II) in an aromatic hydrocarbon and/or alkyl or aralkyl ether solvent at 25-80 degrees C with (III): R1-CHXCOOEt (III) (where X is halogen) in the presence of activated Zn metal (at least 1 mole to 1 mole of (II) and (III), treating the product with hydrazine in excess at 40-60 degrees C for 8-30 hrs. and subjecting the hydrazide to a Curtius rearrangement at =60 degrees C using excess acid and effecting the reaction under a layer of an organic solvent. (I; R=PhCH2CH2, R1=H) is prepd.</p> |
