- 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.
- Wu, Caijiao,Zhou, Qifan,Song, Dake,Li, Hui,Bao, Changshun,Liu, Xuelong,Bao, Xuefei,Chen, Guoliang
-
-
Read Online
- 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.
- Xiong, Yao,Yan, Xilong,Ma, Yawen,Li, Yang,Yin, Guohui,Chen, Ligong
-
-
Read Online
- 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.
- -
-
Paragraph 0021; 0022
(2021/08/21)
-
- 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
- -
-
Paragraph 0027; 0035; 0036
(2019/05/22)
-
- 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.
- -
-
Paragraph 0151
(2018/04/17)
-
- 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.
- -
-
Paragraph 0055; 0056; 0057
(2018/09/08)
-
- 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.
- -
-
Paragraph 0203
(2017/02/09)
-
- 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
- -
-
Paragraph 0016; 0028; 0029
(2017/09/01)
-
- 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.
- -
-
Paragraph 0054; 0055
(2017/12/02)
-
- 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)
- -
-
Paragraph 0051; 0052; 0053
(2017/05/20)
-
- Intermediate of pimavanserin and similar compound thereof, and preparation method thereof, and method for preparing pimavanserin and similar compound thereof
-
The present invention relates to an intermediate of pimavanserin and a similar compound thereof, and a preparation method thereof, and a method for preparing pimavanserin and a similar compound thereof. According to the present invention, the raw materials required by the intermediate have characteristics of low price, easy obtaining, easy separation purification and no requirement of post-treatment, the next step reaction can be directly performed through the one-pot method to prepare the pimavanserin and the similar compound thereof, the operation is simple, and the economical, efficient, safe and environmentally friendly synthesis process is provided for the preparation of the pimavanserin and the similar compound thereof; and with the application of the intermediate to prepare the pimavanserin, the high toxicity and the use of the difficultly-operated phosgene can be avoided, and the total yield of the reaction can achieves the level in the prior art even the higher level.
- -
-
Paragraph 0053; 0056; 0057; 0058; 0059
(2016/10/09)
-
- METHODS FOR THE TREATMENT OF PARKINSON'S DISEASE PSYCHOSIS USING PIMAVANSERIN
-
Methods for the treatment of Parkinson's disease psychosis which comprise the administration of pimavanserin.
- -
-
Paragraph 0066
(2014/06/23)
-
- ANTIBACTERIAL AGENTS: ARYL MYXOPYRONIN DERIVATIVES
-
The invention provides compounds of formula la, lb and Ic: [Formula Ia, Ib, and Ic] and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula Ia-Ic, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.
- -
-
Page/Page column 65
(2014/01/09)
-
- Rational design and synthesis of 4-O-substituted phenylmethylenethiosemicarbazones as novel tyrosinase inhibitors
-
In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have significant tyrosinase inhibitiory activity. Particularly, the IC50 values of compounds 3a-g, 3j and 3s were of the same magnitude as tropolone, one of the best tyrosinase inhibitors known so far. Furthermore, the structure-activity relationships of these compounds were also investigated. All these data suggested that these molecules might be utilized for the development of new candidate for the treatment of dermatological disorders, and further development of such compounds may be of interest.
- Yi, Wei,Cao, Rihui,Chen, Zhiyong,Yu, Liang,Wen, Huan,Yan, Qin,Ma, Lin,Song, Huacan
-
scheme or table
p. 752 - 754
(2010/07/15)
-
- PHENYLALKYLCARBOXYLIC ACID DELIVERY AGENTS
-
The present invention provides phenylalkylcarboxylic acid compounds and compositions containing such compounds which facilitate the delivery of biologically active agents.
- -
-
Page/Page column 37-38
(2008/12/07)
-
- SALTS OF N-(4-FLUOROBENZYL)-N-(1-METHYLPIPERIDIN-4-YL)-N'-(4-(2-METHYLPROPYLOXY)PHENYLMETHYL)CARBAMIDE AND THEIR PREPARATION
-
Disclosed herein are salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide of formula (I) including the citrate, fumarate, maleate, malate, phosphate, succinate, sulphate, and edisylate salts.
- -
-
Page/Page column 21
(2008/06/13)
-
- Competitive formation of β-amino acids, propenoic, and ylidenemalonic acids by the Rodionov reaction from malonic acid, aldehydes, and ammonium acetate in alcoholic medium
-
The Rodionov reaction of 49 available aliphatic and aromatic aldehydes with malonic acid and ammonium acetate in alcoholic medium, resulting in formation of β-amino acids, propenoic, and ylidenemalonic acids, was studied. Certain regioselectivity regularities of the reaction were revealed. Among the variety of ketones studied, cyclohexanone is the only whose reaction yields a β-amino acid. Unusual dehydrofluorination of 6-chloro-2-fluorocinnamic acid under the Rodionov reaction was discovered. 2005 Pleiades Publishing, Inc.
- Lebedev,Lebedeva,Sheludyakov,Kovaleva,Ustinova,Kozhevnikov
-
p. 1113 - 1124
(2007/10/03)
-
- Structure-activity requirements for the antiproliferative effect of troglitazone derivatives mediated by depletion of intracellular calcium
-
Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated by depletion of intracellular calcium stores resulting in inhibition of translation initiation. The unsaturated form of troglitazone displays similar anticancer properties in vitro. In this letter, we report our findings on the minimum structural requirements for both compounds to retain their calcium release and antiproliferative activities.
- Fan, Yun-Hua,Chen, Han,Natarajan, Amarnath,Guo, Yuhong,Harbinski, Fred,Iyasere, Julia,Christ, William,Aktas, Huseyin,Halperin, Jose A.
-
p. 2547 - 2550
(2007/10/03)
-
- Novel sunscreen agents, sunscreen compositions and methods for preventing sunburn
-
The present invention relates to novel sunscreen agents which have the ability to absorb both UVA and UVB wavelength radiation. The sunscreen agents comprise a specific type of UVA-absorbing chromophore covalently bonded to a specific type of UVB-absorbin
- -
-
-
