18962-07-7

Usage

Uses

4-Isobutoxybenzaldehyde to treat neurodegenerative diseases.

InChI:InChI=1/C11H14O2/c1-9(2)8-13-11-5-3-10(7-12)4-6-11/h3-7,9H,8H2,1-2H3

Upstream product

• 78-77-3 Isobutyl bromide 
• 123-08-0 4-hydroxy-benzaldehyde 
• 513-36-0 isobutyryl chloride 
• 513-38-2 Isobutyl iodide 
• 497-19-8 sodium carbonate 
• 1126-75-6 (isobutyloxy)benzene 
• 78-83-1 2-methyl-propan-1-ol 
• 459-57-4 4-fluorobenzaldehyde 
• 100-97-0 hexamethylenetetramine 
• 40141-14-8 4-isobutoxybenzyl chloride 

Downstream Products

• 90672-89-2 (4-Isobutoxy-phenyl)-isothiazol-5-yl-methanol 
• 865137-99-1 3-(chloromethyl)-4-isobutoxybenzaldehyde 
• 639863-75-5 1-(isocyanatomethyl)-4-(2-methylpropoxy)benzene 
• 1080491-31-1 N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N’-(4-(2-methylpropyloxy)phenylmethyl)carbamide tartaric acid 
• 500547-59-1 [4-(2-methylpropoxy)phenyl]methanol 
• 40141-14-8 4-isobutoxybenzyl chloride 
• 21244-29-1 N-(4-isobutoxybenzyl)phthalimide 

Relevant academic research and scientific papers

An improved process for the preparation of pimavanserin tartrate

A practical synthetic route to pimavanserin tartrate, in which the target compound was obtained with 99.84% purity and in 46% total yield via a 5-step synthesis starting from 4-hydroxybenzaldehyde and (4-fluorophenyl)methanamine, is reported. The main advantages of the route include inexpensive starting materials, mild reaction conditions and an acceptable overall yield.

Regulating the piezofluorochromism of 9,10-bis(butoxystyryl)anthracenes by isomerization of butyl groups

Isomers of 9,10-bis(butoxystyryl)anthracene (DSA4), including n-butyl, i-butyl and t-butyl at ortho or para positions, were designed and synthesized. All of them display an aggregation-induced emission phenomenon. Remarkably, it was found that isomerization of butyl endgroups presents significant influences on their piezofluorochromic properties. Thus, an alternative approach to design and obtain piezofluorochromic compounds is proposed here.

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.

A high-purity matching not fan selin preparation method

The invention belongs to the technical field of pharmaceutical and chemical industries, and in particular relates to a high-purity matching not fan selin preparation method. The present invention provides a high-purity matching not fan selin preparation m

PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF PIMAVANSERIN

The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.

Pimavanserin intermediate and preparation method of pimavanserin

The invention discloses a pimavanserin intermediate and a preparation method of pimavanserin. A structural general formula of the pimavanserin intermediate is shown in the description; the pimavanserin intermediate is prepared by carrying out reductive amination on 4-isobutoxybenzaldehyde and carbamate; a synthesis route is shown in the description; the pimavanserin is obtained through ammonolysisreaction. According to the preparation method of the pimavanserin intermediate, the target intermediate is obtained in one step through reductive amination reaction and reaction steps of the pimavanserin are extremely simplified; used raw materials are safe and the cost is low; reaction conditions are moderate and phosgene which has great toxicity and is uneasy to operate is not used, so that thepreparation method is easy to realize in industry; the intermediate and a product are easy to separate and purify, and the next-step reaction can be directly carried out to prepare the pimavanserin,without the need of separating the pimavanserin; the preparation method is simple to operate and the yield is higher than that of the prior art; the synthesis cost of the pimavanserin is reduced.

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-(l-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-fluorobenzyl)-N-(l-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt.

Synthesis method for pimavanserin intermediate

The invention discloses a synthesis method for a pimavanserin intermediate. The synthesis method comprises the steps of firstly allowing 4-hydroxybenzaldehyde to react with iso-butyl bromide to obtain 4-isobutoxybenzaldehyde as an initial raw material; an

Tartaric acid pimavanserin impurities and preparation method thereof

The invention discloses tartaric acid pimavanserin impurities, namely N-(4-isobutoxy benzyl) diphenyl aminodiphthalate (impurity A), 4-isobutoxy benzyl carbonic acid phenyl ester (impurity B), 4-fluorobenzyl (1-methylpiperidine-4-yl) carbonic acid-4-isobutoxy benzyl ester (impurity C) and N-( isobutoxy benzyl)-N'-(4-fluorobenzyl) urea (impurity E). In addition, the invention further discloses a preparation method of tartaric acid pimavanserin impurities A, B, C and E and an N,N'-bis(4-isobutoxy benzyl) urea (impurity D). Through application of the tartaric acid pimavanserin impurities as reference substances in research on the quality of the tartaric acid pimavanserin intermediate, a crude drug and a compound preparation thereof, a solid foundation is laid for research on the quality of tartaric acid pimavanserin.

Isoglycyrrhiza derivatives and its use (by machine translation)

The invention discloses a different of glycyrrhizin derivatives and their use, the structure of the isoliquiritigenin main body: wherein R 1 is H, methyl, cyclopropane methyl, 3-methyl-2-butenyl, is d acyl, alkyl in the isobutene, R 2 is H, methyl, cyclopropane methyl, 3-methyl-2-butenyl, is d acyl, alkyl of isobutene. Said compound can be used for the treatment of atrial fibrillation, and is capable of effectively inhibiting potassium channel function of the patient and small side effect. (by machine translation)