METHODS FOR PREPARING N-(4-FLUOROBENZYL)-N-(1-METHYLPIPERIDIN-4-YL)-N'-(4-(2-METHYLPROPYLOXY)PHENYLMETHYL)CARBAMIDE AND ITS TARTRATE SALT AND POLYMORPHIC FORM
First Claim
1. A method of preparing pimavanserin (N-(4-fluorophenylmethyl)-N-(1 -methylpiperidin-4-yl)-N′
- -(4-(2-methylpropyloxy)phenylmethyl)carbamide) or a salt thereof, the method comprising;
contacting an intermediate according to Formula (A2),
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Abstract
Disclosed herein are methods for obtaining N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl) carbamide (pimavanserin) comprising the step of contacting an intermediate according to Formula (A) or a salt thereof, with an intermediate Formula B, or a salt thereof, to produce pimavanserin or a salt thereof wherein Y is —ORi or —NR2aR2b; R3 is hydrogen or substituted or unsubstituted heteroalicyclyl, R4 is substituted or unsubstituted aralkyl; X is —OR22 or —NR23R24; (wherein R22 is hydrogen or substituted or unsubstituted C1-6alkyl and one of R23 and R24 is hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and R21 is —OCH2CH(CH3)2 or F; Also disclosed herein is the tartrate salt of N-(4-fluoroben-zyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt.
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Citations
27 Claims
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1. A method of preparing pimavanserin (N-(4-fluorophenylmethyl)-N-(1 -methylpiperidin-4-yl)-N′
- -(4-(2-methylpropyloxy)phenylmethyl)carbamide) or a salt thereof, the method comprising;
contacting an intermediate according to Formula (A2), - View Dependent Claims (11, 12, 13, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27)
- -(4-(2-methylpropyloxy)phenylmethyl)carbamide) or a salt thereof, the method comprising;
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2-10. -10. (canceled)
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14. (canceled)
Specification