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US 2001/0018538 A1Published application
New process for a phenylthiobutyl-isoquinoline and intermediates therefor
AssigneeHoffmann-La Roche Inc.
InventorHans Hilpert
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Abstract
A method for making phenylthiobutyl-isoquinoline compounds of formula 1 and novel intermediates therefor.
Claims25
A method for making a compound of formula 13
- wherein R1 is lower alkyl or benzyl and X is halogen,
- which process comprises
- (a) silylating a carbamate group of a compound of formula 14
- wherein R is lower alkyl and R1 is lower alkyl or benzyl,
- to form a silyl-protected compound;
- and
- (b) alkylating the silyl-protected compound in the presence of dihalogenated methane with a lower-alkyl-lithium to produce the compound of formula VI.
4 more elements
A method for making a compound of formula V 16
- comprising treating a compound of formula VI 17
- wherein R1 is methyl or ethyl and X is halogen,
- with a reducing agent selected from the group consisting of an aluminium trialkoxide and lithium aluminium trialkoxyhydride to yield the halogen alcohol of formula V.
A compound of formula 18
- wherein R is lower alkyl and R1 is lower alkyl.
A compound of formula 19
- wherein R is lower alkyl, R1 is lower alkyl, and R2, R3 and R4 are lower-alkyl or phenyl.
A compound of formula 20
- wherein R is lower alkyl, R1 is lower alkyl, and R2, R3 and R4 are lower-alkyl or phenyl.
A compound of formula 21
- wherein R1 is lower alkyl and X is halogen.
A compound of formula 22
- wherein R1 is lower alkyl and X is halogen.
A compound of formula 23
- wherein R1 is lower alkyl.
A compound of formula 24
- wherein R1 is lower alkyl.
Dependencies are inferred from the claim text.