359878-47-0

Usage

Uses

Used in Pharmaceutical Industry:
N-[(4-Fluorophenyl)methyl]-1-methyl-4-piperidinamine is used as a pharmaceutical intermediate for the synthesis of various drugs. Its unique structure allows it to serve as a building block in the development of new medications, particularly those targeting the central nervous system.
As a pharmaceutical intermediate, N-[(4-Fluorophenyl)methyl]-1-methyl-4-piperidinamine is utilized for the following reasons:
1. Its fluorophenyl group can potentially enhance the lipophilicity and bioavailability of the final drug product, improving its absorption and distribution within the body.
2. The presence of the methyl group on the first carbon can influence the compound's metabolic stability and pharmacokinetic properties, which are crucial factors in drug design.
3. The piperidine ring provides a versatile scaffold for further chemical modifications, allowing the development of a range of drug candidates with different therapeutic applications.

InChI:InChI=1/C13H19FN2/c1-16-8-6-13(7-9-16)15-10-11-2-4-12(14)5-3-11/h2-5,13,15H,6-10H2,1H3

Upstream product

• 1445-73-4 1-Methyl-4-piperidone 
• 140-75-0 para-fluorobenzylamine 
• 41838-46-4 4-Amino-1-methylpiperidine 
• 459-57-4 4-fluorobenzaldehyde 

Downstream Products

• 1080491-34-4 1-(4-fluorobenzyl)-3-(4-(1,1-d2-isobutoxy)benzyl)-1-(1-methylpiperidin-4-yl)urea 
• 1246458-38-7 3-(4-(benzyloxy)-2-methoxybenzyl)-1-(4-fluorobenzyl)-1-(1-methylpiperidin-4-yl)urea 
• 1246458-14-9 methyl 3-(4-((3-(4-fluorobenzyl)-3-(1-methylpiperidin-4-yl)ureido)methyl)phenoxy)-2-methylpropanoate 
• 1246458-36-5 3-(2-(benzyloxy)-4-methoxybenzyl)-1-(4-fluorobenzyl)-1-(1-methylpiperidin-4-yl)urea 
• 1246458-29-6 1-(4-fluorobenzyl)-3-(3-benzyloxy-4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea 
• 1246458-13-8 1-(4-fluorobenzyl)-3-(4-(2-methylallyloxy)benzyl)-1-(1-methylpiperidin-4-yl)urea 
• 706779-91-1 N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N′-(4-(2-methylpropyloxyl)phenylmethyl)carbamide 
• 1080491-31-1 N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N’-(4-(2-methylpropyloxy)phenylmethyl)carbamide tartaric acid 
• 955997-87-2 N,N'-bis(4-isobutoxybenzyl)urea 
• 706782-28-7 Pimavanserin tartrate 

Relevant academic research and scientific papers

Novel derivatives of urea and use thereof

The present invention relates to a novel urea derivative compound and 5HT thereof. 2A The present invention relates to the use of antagonists as antagonists for the prevention or treatment of neuropsychiatric disorders, degenerative brain diseases, propagated disorders and/or metabolic diseases.

Preparation method and application of 4-(4-fluorobenzylamino)-1-methylpiperidine

The invention relates to a preparation method of 4-(4-fluorobenzylamino)-1-methylpiperidine, which comprises the following steps: by taking lithium borohydride as a reducing agent, tetrahydrofuran as a reaction system and ammonium chloride as a catalyst, p-fluorobenzylamine and N-methyl-4-piperidone are added for reaction to obtain a crude product with the content of 95% or above; the high-purity product with the purity of 99% is obtained through tower plate rectification, almost no impurity exists, powerful help is provided for subsequent API purification, and the yield is high. The reducing agent is low in price and can be industrially produced, so that the production cost of the product is effectively reduced.

Application of pimavanserin in preparation of antitumor drugs

The invention relates to application of pimavanserin in preparation of antitumor drugs, belongs to the technical field of medicines, and particularly relates to novel application of pimavanserin in preparation of antitumor drugs. The structural formula of the pimavanserin is shown in the formula I. The biological activity test of the compound shows that the compound has antitumor activity and is a novel antitumor drug.

Design, Synthesis, and Biological Evaluation of New Peripheral 5HT2A Antagonists for Nonalcoholic Fatty Liver Disease

Nonalcoholic fatty liver disease (NAFLD) is increasingly prevalent worldwide, causing serious liver complications, including nonalcoholic steatohepatitis. Recent findings suggest that peripheral serotonin (5-hydroxytryptamine, 5HT) regulates energy homeostasis, including hepatic lipid metabolism. More specifically, liver-specific 5HT2A knockout mice exhibit alleviated hepatic lipid accumulation and hepatic steatosis. Here, structural modifications of pimavanserin (CNS drug), a 5HT2A antagonist approved for Parkinson's disease, led us to synthesize new peripherally acting 5HT2A antagonists. Among the synthesized compounds, compound 14a showed good in vitro activity, good liver microsomal stability, 5HT subtype selectivity, and no significant inhibition of CYP and hERG. The in vitro and in vivo blood-brain barrier permeability study proved that 14a acts peripherally. Compound 14a decreased the liver weight and hepatic lipid accumulation in high-fat-diet-induced obesity mice. Our study suggests new therapeutic possibilities for peripheral 5HT2A antagonists in NAFLD.

PROCESS FOR THE MANUFACTURING OF PIMAVANSERIN

The present invention relates to a new process for manufacturing 1-(4-fluorobenzyl)-3-(4-iso-butoxyphenyl)-1-(1-methylpiperidin-4-yl)urea, with the INN name pimavanserin, and its hemitartrate salt.

Preparation method of pimavanserin solid intermediate

The invention relates to the field of chemical medicines, in particular to a preparation method of a pimavanserin solid intermediate. The solid intermediate prepared by the preparation method is highin purity, and the preparation method is simple in operation and suitable for industrial large-scale production.

A PHARMACEUTICAL INTERMEDIATE

This invention relates to4-(4-fluorobenzylamino)-1-methylpiperidine trihydrateand a process for the preparation of 4-(4-fluorobenzylamino)-1-methylpiperidine trihydrate comprising treating 4-(4- fluorobenzylamino)-1-methylpiperidine with water. The invention also relates toa process for the preparation of pimavanserin comprising reacting 4-(4- fluorobenzylamino)-1-methylpiperidine trihydrate with 1-isobutoxy-4-(isocyanatomethyl)benzene; toa process for the preparation of a pimavanserin acid addition salt comprising reacting 4-(4- fluorobenzylamino)-1-methylpiperidine trihydrate with 1-isobutoxy-4-(isocyanatomethyl)benzene and converting pimavanserin into a pimavanserinacid additionsalt, pimavanserin and pimavanserin acid addition salts obtainable by the process, and to the use of 4-(4-fluorobenzylamino)-1-methylpiperidine trihydrate for preparing pimavanserin or an acid additionsalt thereof.

COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES

The present disclosure relates to compounds according to Formulae (I), (II) and (VIII), useful for treating diseases.

COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES

The present disclosure relates to compounds according to Formula (I), useful for treating diseases.