US2005020670A1PendingUtilityA1
Stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofuran
Est. expiryMar 13, 2020(expired)· nominal 20-yr term from priority
A61P 43/00A61P 9/10A61P 25/28A61P 25/24C07D 307/87C07D 263/52C07D 413/04C07D 277/60C07D 263/10C07D 277/10C07D 417/04A61K 31/343
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Claims
Abstract
Methods for manufacture of citalopram through stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans are disclosed.
Claims
exact text as granted — not AI-modified1 - 21 . (Canceled)
22 . A compound of the formula V
wherein R represents CN, OH, O-triflate, halogen, NHR 5 wherein R 5 is selected from hydrogen and C 1-6 alkylcarbonyl, CHO, CO 2 R 6 , CONHR 7 wherein R 6 —R 7 are each independently selected from hydrogen and C 1-6 alkyl, or R is a oxazoline or a thiazoline of the formula
wherein U is O or S;
R 1 -R 2 are each independently selected from hydrogen and C 1-6 alkyl, or R 1 and R 2 together form a C 2-5 alkylene chain thereby forming a spiro ring; R 3 is selected from hydrogen and C 1-6 alkyl, R 4 is selected from hydrogen, C 1-6 alkyl, a carboxy group or a precursor group therefor, or R 3 and R 4 together form a C 2-5 alkylene chain thereby forming a spiro ring.
23 . A compound according to claim 22 , wherein R represents CN.
24 . A compound of the formula VI
wherein R represents CN, OH, O-triflate, halogen, NHR 5 wherein R 5 is selected from hydrogen and C 1-6 alkylcarbonyl, CHO, CO 2 R 6 , CONHR 7 wherein R 6 —R 7 are each independently selected from hydrogen and C 1-6 alkyl, or R is a oxazoline or a thiazoline of the formula
wherein U is O or S;
R 1 -R 2 are each independently selected from hydrogen and C 1-6 alkyl, or R 1 and R 2 together form a C 2-5 alkylene chain thereby forming a spiro ring; R 3 is selected from hydrogen and C 1-6 alkyl; R 4 is selected from hydrogen, C 1-6 alkyl, a carboxy group or a precursor group therefor, or R 3 and R 4 together form a C 2-5 alkylene chain thereby forming a spiro ring.
25 . A compound of the formula VII
wherein R represents CN, OH, O-triflate, halogen, NHR 5 wherein R 5 is selected from hydrogen and C 1-6 alkylcarbonyl, CHO, CO 2 R 6 , CONHR 7 wherein R 6 -R 7 are each independently selected from hydrogen and C 1-6 alkyl, or R is a oxazoline or a thiazoline of the formula
wherein U is O or S;
R 1 -R 2 are each independently selected from hydrogen and C 1-6 alkyl, or R 1 and R 2 together form a C 2-5 alkylene chain thereby forming a spiro ring; R 3 is selected from hydrogen and C 1-6 alkyl; R 4 is selected from hydrogen, C 1-6 alkyl, a carboxy group or a precursor group therefor, or R 3 and R 4 together form a C 2-5 alkylene chain thereby forming a spiro ring.
26 . A compound of the formula VIII
wherein R represents CN, OH, O-triflate, halogen, NHR 5 wherein R 5 is selected from hydrogen and C 1-6 alkylcarbonyl, CHO, CO 2 R 6 , CONHR 7 wherein R 6 -R 7 are each independently selected from hydrogen and C 1-6 alkyl, or R is a oxazoline or a thiazoline of the formula
wherein U is O or S;
R 1 -R 2 are each independently selected from hydrogen and C 1-6 alkyl, or R 1 and R 2 together form a C 2-5 alkylene chain thereby forming a spiro ring; R 3 is selected from hydrogen and C 1-6 alkyl; R 4 is selected from hydrogen, C 1-6 alkyl, a carboxy group or a precursor group therefor, or R 3 and R 4 together form a C 2-5 alkylene chain thereby forming a spiro ring.Join the waitlist — get patent alerts
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