CAS: 359878-47-0; 4-(4-Fluorobenzylamino)-1-Methylpiperidine

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CAS号1445-73-4 N-甲基-4-哌啶酮 | CAS号140-75-0 对氟苄胺 | CAS号706779-91-1 2-胺基-5-(4-硝基苯磺酰)-噻唑

N-甲基-4-哌啶酮,对氟苄胺置于sodium Cyanoborohydride,溶剂黄146体系中,用 异丙醇 作为反应溶剂,以90 %的收率获得产物n-(4-氟苄基)-1-甲基哌啶-4-胺
参考文献:作为潜在血清素 5-Ht2A 受体反向激动剂的新型 Pimavanserin 类似物的设计,合成,分子对接和生物学评价
标题:作为潜在血清素 5-Ht2A 受体反向激动剂的新型 Pimavanserin 类似物的设计,合成,分子对接和生物学评价
摘要:人们担心使用第二代抗精神病药物治疗帕金森病精神病(pdp)和痴呆相关精神病会产生重要的副作用.pimavanserin 是唯一被授权用于 Pdp 的抗精神病药物,代表 5-Ht 2A受体 (5-Ht2Ar)的反向激动剂,对多巴胺受体缺乏亲和力.因此,开发无多巴胺能活性的血清素5-Ht2Ar反向激动剂对不同的神经精神疾病来说是一个挑战.通过基于配体的药物设计,我们发现了匹马范色林类似物的新结构(2,3和4).体外竞争性受体结合和功能性 G 蛋白偶联测定表明化合物2,图3和4在人脑皮质和重组细胞中显示出比匹马范色林作为5-Ht2Ar反向激动剂更高的效力.为了评估分子取代基对 5-Ht2Ar 的选择性和反向激动作用的影响,进行了分子对接和计算机预测的物理化学参数.对接研究与体外筛选一致,结果与匹马范色林相似.
DOI:10.1021/acs.Jmedchem.3C00662

专利信息

专利号:US-8236960-B2
优先权日:2004-09-27
标 题 :Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy) phenylmethyl)carbamide and its tartrate salt and crystalline forms
发明人：THYGESEN MIKKEL BOAS; SCHLIENGER NATHALIE; TOLF BO-RAGNAR; ANDERSSON CARL-MAGNUS A; BLATTER FRITZ; BERGHAUSEN JOERG
权利人:THYGESEN MIKKEL BOAS; SCHLIENGER NATHALIE; TOLF BO-RAGNAR; ANDERSSON CARL-MAGNUS A; BLATTER FRITZ; BERGHAUSEN JOERG; ACADIA PHARM INC
摘要:Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl) -N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2 -methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.

专利号:US-11319288-B2
优先权日:2018-04-26
标 题:Method for the preparation of pimavanserin base
发明人：NOVO BARBARA; BONANOMI JACOPO; BERTOLOTTI MATTIA
权利人:OLON SPA
摘要:Disclosed is a process for the synthesis of pimavanserin base with a high yield and purity, which comprises: a) converting tert-butyl-N-[(4-propan-2-yloxyphenyl)methyl]carbamate (Formula (I)) to 1-(isocyanatomethyl)-4-propan-2-yloxybenzene of formula (II) b) adding N-[(4-fluorophenyl)methyl]-1-methylpiperidin-4-amine (Formula (IV)) to the solution obtained in a) to give pimavanserin base, and c) purifying the pimavanserin base obtained in step b).

专利号:US-7790899-B2
优先权日:2004-09-27
标 题 :Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
发明人：TOLF BO-RAGNAR; SCHLIENGER NATHALIE; THYGESEN MIKKEL BOAS
权利人:ACADIA PHARM INC
摘要:Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.

专利号:US-10807953-B2
优先权日:2015-03-02
标题:Processes and intermediates for the preparation of Pimavanserin
发明人：BILJAN TOMISLAV; DOGAN JASNA; METSGER LEONID; PIPERCIC SARA MORASI; RATKAJ MARINA; SKUGOR MAJA MATANOVIC; WANG YI
权利人:PLIVA HRVATSKA D O O
摘要: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.

专利号:US-2006205780-A1
优先权日:2004-09-27
标 题 :Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms

专利号:US-2006205781-A1
优先权日:2004-09-27
标 题 :Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms