BASIC ETHERS OF 1-PHENYL-2-(2-THIENYL)ETHANOLS

• Main Authors: CROSS P,GB, DICKINSON R,GB
• Format: Patent
• Language: English
• Published: 04.06.1974
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

1342520 Alkyl-substituted-benzyl- or -thenylbenzyloxy derivatives of amines PFIZER Ltd 13 July 1972 [14 July 1971] 32956/71 Heading C2C Novel compounds (I) (including salts and optical isomers thereof) where It is H is halogen at the 3- or 4-position ; R1 signifies a group (II) or (III) wherein R2 represents an alkyl group containing from 3 to 5 carbon atoms; and Y represents either (A) an aminoalkyl group of the formula in which R3 and R4 each represent a C 1 to C 4 alkyl group or together with the nitrogen atom to which they are attached form a saturated heterocyclic group, and "Alk" represents a divalent saturated aliphatic hydrocarbon group containing from 2 to 4 carbon atoms, the free valences being located on different carbon atoms; or (B) an amino-cyclic group of the formula -CnH 2 n-CHZ, in which n is 0 to 3 and Z is a divalent group which completes a saturated heterocyclic ring containing at least one nitrogen atom and at least 4 carbon atoms, any such nitrogen atom being separated from the oxygen atom to which the amino-cyclic group is attached by a chain of from 2 to 4 carbon atoms; are made by standard methods starting from compounds (IV). The following compounds are also prepared: DL - 1 - benzyl - 4[2 - (5 - neopentyl - 2 - thienyl). 1 - phenyl] - ethoxyacetyl - piperazine and the precursors therefor, i.e. the corresponding- ethoxyacetyl chloride and -ethoxyacetic acid and ethyl ester of said acid. Pharmaceutical preparations having antihistamine action contain (I) as active ingredient; administration may be orally or parenterally.