تفاعل #1667310

ord-d213f94bfbaa4b38b83e37cc7d1226cb

معادلة التفاعل

Br.c1cc[nH+]cc1
pyridinium hydrobromide
COc1cccc(C2(C(N)=O)CCC(=O)C(Br)C2)c1
2-bromo-4-(3-methoxyphenyl)-4-carbamoyl-cyclohexanone
COc1cccc(C2(C(N)=O)CCC(=O)CC2)c1
4-(3-methoxyphenyl)-4-carbamoyl-cyclohexanone
BrBr
bromine
NC(=O)C1CCCCC1
carbamoyl-cyclohexane
Cl
hydrochloric acid
O=S(=O)(O)O
sulfuric acid
COc1cccc(C23CCC(=O)C(C2)NC3=O)c1
1-(3-methoxyphenyl)-6-azabicyclo[3,2,1]octane-4,7-dione

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىat room temperature
  2. 2
    أخرىat room temperature

الإجراء التجريبي

First of all, 1-(3-methoxyphenyl)-6-azabicyclo[3,2,1]-octane-7-one (VIII) is prepared by the six steps of (I) hydrolyzing 4-(3-methoxyphenyl)-4-cyano-1,1,-ethylenedioxy-cyclohexane (VII) with an alkali metal hydroxide(e.g., sodium hydroxide, potassium hydroxide) under heating in a solvent (e.g., methanol, ethanol, ethyleneglycol, a mixture of one of these solvents and water) to give 4-(3-methoxyphenyl)-4-carbamoyl-1,1-ethylenedioxy-cyclohexane, (2) reacting said carbamoyl-cyclohexane with an acid(e.g., hydrochloric acid, sulfuric acid, acetic acid) under heating, (3) brominating the resultant 4-(3-methoxyphenyl)-4-carbamoyl-cyclohexanone with bromine or pyridinium hydrobromide perbromide (C5H5N+HBr-) at room temperature in a solvent (e.g., acetic acid, tetrahydrofuran), (4) reacting the resultant 2-bromo-4-(3-methoxyphenyl)-4-carbamoyl-cyclohexanone with an alkali metal hydride (e.g., sodium hydride) or an alkali metal alkoxide (e.g., sodium methoxide, potassium methoxide, sodium ethoxide, potassium ethoxide) at room temperature in a solvent(e.g., methanol, ethanol, dimethoxyethane) to give 1-(3-methoxyphenyl)-6-azabicyclo[3,2,1]octane-4,7-dione, (5) refluxing a mixture of said product and hydrazine hydrate under heating in a solvent (e.g., ethanol, ethyleneglycol), and then (6) heating the resultant 1-(3-methoxyphenyl)-6-azabicyclo[3,2,1]octane-4,7-dione-4-hydrazone in the presence of an alkali agent(e.g., potassium hydroxide, potassium tert.-butoxide) in a solvent (e.g., toluene).

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US03932429uspto-grants-1976_01