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 —OR.sub.i or —NR.sub.2aR.sub.2b; R.sub.3 is hydrogen or substituted or unsubstituted heteroalicyclyl, R.sub.4 is substituted or unsubstituted aralkyl; X is —OR.sub.22 or —NR.sub.23R.sub.24; (wherein R.sub.22 is hydrogen or substituted or unsubstituted C.sub.1-6alkyl and one of R.sub.23 and R.sub.24 is hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and R.sub.21 is —OCH.sub.2CH(CH.sub.3).sub.2 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. ##STR00001##

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 —OR.sub.i or —NR.sub.2aR.sub.2b; R.sub.3 is hydrogen or substituted or unsubstituted heteroalicyclyl, R.sub.4 is substituted or unsubstituted aralkyl; X is —OR.sub.22 or —NR.sub.23R.sub.24; (wherein R.sub.22 is hydrogen or substituted or unsubstituted C.sub.1-6alkyl and one of R.sub.23 and R.sub.24 is hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and R.sub.21 is —OCH.sub.2CH(CH.sub.3).sub.2 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. ##STR00001##

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 —OR.sub.i or —NR.sub.2aR.sub.2b; R.sub.3 is hydrogen or substituted or unsubstituted heteroalicyclyl, R.sub.4 is substituted or unsubstituted aralkyl; X is —OR.sub.22 or —NR.sub.23R.sub.24; (wherein R.sub.22 is hydrogen or substituted or unsubstituted C.sub.1-6alkyl and one of R.sub.23 and R.sub.24 is hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and R.sub.21 is —OCH.sub.2CH(CH.sub.3).sub.2 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. ##STR00001##

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 —OR.sub.i or —NR.sub.2aR.sub.2b; R.sub.3 is hydrogen or substituted or unsubstituted heteroalicyclyl, R.sub.4 is substituted or unsubstituted aralkyl; X is —OR.sub.22 or —NR.sub.23R.sub.24; (wherein R.sub.22 is hydrogen or substituted or unsubstituted C.sub.1-6alkyl and one of R.sub.23 and R.sub.24 is hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and R.sub.21 is —OCH.sub.2CH(CH.sub.3).sub.2 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. ##STR00001##

The present disclosure discloses a method for safely preparing pimavanserin and tartrate thereof by using triphosgene. The synthesis route includes: ##STR00001##
Raw materials used in the method of the present disclosure are safe and inexpensive, thereby effectively reducing the production costs. The method of the present disclosure has mild reaction conditions, and avoids using phosgene, which is highly toxic and difficult to handle is avoided. Thus, the method is readily implemented industrially.

The present disclosure discloses a method for safely preparing pimavanserin and tartrate thereof by using triphosgene. The synthesis route includes: ##STR00001##
Raw materials used in the method of the present disclosure are safe and inexpensive, thereby effectively reducing the production costs. The method of the present disclosure has mild reaction conditions, and avoids using phosgene, which is highly toxic and difficult to handle is avoided. Thus, the method is readily implemented industrially.

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

This disclosure relates to aryl amidines of Formula I and their use as fungicides.

##STR00001##

This disclosure relates to aryl amidines of Formula I and their use as fungicides.

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