反応 #215853

反応方程式

oxazepine-10(11H)-carbonyl chloride

8-chlorodibenz[b,f][1,4]-oxazepine-10(11H)carbonyl chloride

HCl

8-chlorodibenz[b,f][1,41oxazepine-10(11H)-carboxylic acid, 2-[1-oxo-3-(2-pyridinyl)propyl]hydrazide

α,α-difluoro-β-hydroxy-3-(4-pyridinyl)-propanoic acid, hydrazide

→

8-chlorodibenz[b,f][1,4]oxazepine-10(11H)carboxylic acid, 2-[2,2-difluoro-3-hydroxy-1-oxo-3-(4-pyridinyl)propyl]hydrazide

溶媒

acetic acid

反応条件

後処理

1. 1
   その他prepared in the manner
2. 2
   その他prepared in the manner

実験手順

The free base of 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)carboxylic acid, 2-[2,2-difluoro-3-hydroxy-1-oxo-3-(4-pyridinyl)propyl]hydrazide (51) was prepared in the same manner as 8-chlorodibenz[b,f][1,41oxazepine-10(11H)-carboxylic acid, 2-[1-oxo-3-(2-pyridinyl)propyl]hydrazide (6), as described above in Example 6, on a 1.75 mmol scale from α,α-difluoro-β-hydroxy-3-(4-pyridinyl)-propanoic acid, hydrazide (50), prepared in the manner described above in Example 50, and 8-chlorodibenz[b,f]8 1,4]-oxazepine-10(11H)-carbonyl chloride (2), prepared in the manner described above in Example 2, for a yield of 0.098 g (12%) of product. The free base was taken up in acetic acid 1.5 mL) and 1M HCl (1.5 mL). The material was lyophilized to yield 0.049 mg of the hydrochloride salt. Analysis calculated for C22H17N4O4F2Cl.HCl.0.25 H2O (M.W. 514.83): C, 51.23; H, 3.62; N, 10.86. Found: C, 50.85; H, 3.67; N, 10.94.

出典