| 摘要 |
<p>A process for producing a hydrazide of formula (1.0) is disclosed. The process comprises reacting a hydrazone of formula (2.0) or (2.1), wherein said hydrazone is in toluene, with a mixture of Grignard reagents, wherein said Grignard reagents are in a suitable organic solvent; wherein: (A) Z is a suitable carbonyl protecting group; (B) R is a suitable -OH protecting group; (C) R<1> is selected from: H, a non-enolizable alkyl, a non-enolizable substituted alkyl, aryl, substituted aryl, -S-aryl, -S-(substituted aryl), -S-alkyl, -S-(substituted alkyl), alkoxy, substituted alkoxy, aryloxy, or substituted aryloxy; (D) said mixture of Grignard reagents comprises R<2>MgX in admixture with R<3>MgX; (E) R<2> is a suitable alkyl, substituted alkyl, alkenyl, alkynyl, aryl, substituted aryl, or aralkyl group capable of adding to the -C=N group of the hydrazone to produce the hydrazide; (F) R<3> is a suitable alkyl, substituted alkyl, aryl or substituted aryl group that is more sterically hindered than said R<2> group; (G) X is independently selected from Cl, Br or I for each Grignard reagent; (H) when said hydrazone is a compound of formula (2.0) then the reaction is conducted at a temperature of about +30 to about -40 DEG C; and (I) when said hydrazone is a compound of formula (2.1) then the reaction is conducted at a temperature of about +40 to about -20 DEG C.</p> |
