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US 2003/0120081 A1Published application
Process for the preparation of non-steroidal glucocorticoid receptor modulators
AssigneesPfizer Inc., Pfizer Products Inc.
InventorsJerry A. Murry, Timothy D. White
Life of this patent
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Abstract
A process for preparing a compound of the formula 1 useful as a non-steroidal glucocorticoid receptor modulator.
Claims28
A process for preparing a compound of the formula
- 71
- comprising reacting a compound of the formula
- 72
- with an amide of the formula
- 73
- in the presence of 1,1′-carbonyldiimazole.
3 more elements
A process for preparing a compound of the formula
- 90
- comprising (a) reacting a compound of the formula
- 91
- with pyrrolidine followed by reacting the resultant pyrrolidine enamine intermediate with a benzyl halide to form the compound of formula IX
- 92
- (b) reacting the compound of formula IX so formed with methyl vinyl ketone to form the compound of formula VIII
- 93
- (c) reacting the compound of formula VIII so formed with sodium methoxy to form the compound of formula VII
- 94
- (d) reacting the compound of formula VII so formed with a cyanide source in the presence of a catalyst to form the compound of formula VI
- 95
- (e) reducing the compound of formula VI so formed with hydrogen in the presence of a catalyst and potassium chloride to form the compound of formula V
- 96
- (f) reacting the compound of formula V so formed with trifluoromethylpropyne to form the compound of formula IV
- 97
- (g) reducing the compound of formula IV so formed with hydrogen in the presence of a catalyst to form the compound of formula III
- 98
- (h) reacting the compound of formula III so formed with aqueous sodium hydroxide in a polar protic solvent to form the compound of formula II
- 99
- (ii) reacting the compound of formula II so formed with an amide of the formula
- 100
- in the presence of 1,1′-carbonyldiimazole.
19 more elements
A process for preparing a compound of the formula
- 101
- comprising reacting the compound of the formula
- 102
- with methyl vinyl ketone.
1 more element
A process for preparing a compound of the formula
- 108
- comprising reacting the compound of the formula
- 109
- with a borane or a borate.
1 more element
A process for preparing a compound of the formula
- 110
- comprising reacting a compound of the formula
- 111
- with a compound of the formula
- 112
2 more elements
A process for preparing a compound of the formula
- 115
- comprising reacting a compound of the formula
- 116
- with an amine of the formula
- 117
- in the presence of 1,1′carbonydiimidazole.
3 more elements
A compound of the formula
- 128
A compound of the formula
- 129
A compound of the formula
- 130
A compound of the formula
- 131
A compound of the formula
- 132
A compound of the formula
- 133
Dependencies are inferred from the claim text.