Acadia Pharmaceuticals Inc.

Andreas Philipp Boudier

Beat Theodor Weber

Marlon Carlos

Roger Olsson

Mikael Hillgren

Sagun Tandel

Matthew J Fleming

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 &#x2014;ORor &#x2014;NRR; Ris hydrogen or substituted or unsubstituted heteroalicyclyl, Ris substituted or unsubstituted aralkyl; X is &#x2014;ORor &#x2014;NRR; (wherein Ris hydrogen or substituted or unsubstituted Calkyl and one of Rand Ris hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and Ris &#x2014;OCHCH(CH)or F; Also disclosed herein is the tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt.

Methods for preparing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form c

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 &#x2014;ORor &#x2014;NRR; Ris hydrogen or substituted or unsubstituted heteroalicyclyl, Ris substituted or unsubstituted aralkyl; X is &#x2014;ORor &#x2014;NRR; (wherein Ris hydrogen or substituted or unsubstituted Calkyl and one of Rand Ris hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and Ris &#x2014;OCHCH(CH)or F; Also disclosed herein is the tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N&#x2032;-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt. 

Methods for preparing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form

Methods for preparing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form C

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Zurich, Switzerland

Andreas Philipp Boudier