CAS: 55455-92-0; 1-(3-Phenylpropyl)Piperazine

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CAS号18903-01-0 N-肉桂基哌嗪 | CAS号110-85-0 哌嗪 | CAS号104-52-9 3-苯基-1-氯丙烷 | CAS号637-59-2 1-溴-3-苯基丙烷 | CAS号117132-90-8 1-(3-phenylprop... | CAS号645-45-4 3-苯丙酰氯 | CAS号59698-38-3 4-(3-phenyl-pro... | CAS号501-52-0 3-苯丙酸 | CAS号7542-23-6 piperazinium ch... | CAS号67469-69-6 伐诺司林 | CAS号67469-78-7 伐诺司林二盐酸盐 | CAS号165377-43-5 Cutamesine

📜1-氯-3-苯基丙烷置于potassium Carbonate,三氟乙酸,Sodium Iodide体系中,用 二氯甲烷,乙腈 作为反应溶剂,化学反应 24.0H,反应生成 苯基丙基哌嗪
参考文献:1,4-二取代哌嗪和哌啶作为三重再摄取抑制剂的设计,合成和体外活性.
标题:1,4-二取代哌嗪和哌啶作为三重再摄取抑制剂的设计,合成和体外活性.
摘要:单胺转运蛋白调节着单胺神经递质的浓度,这对于重要的生理过程至关重要,其功能障碍会导致多种中枢神经系统疾病.目前,单胺转运蛋白似乎是这些疾病管理中的潜在靶标.在这项研究中,同源性和生物立体异构技术已被用于设计新的1,4-二取代哌嗪和哌啶.这些衍生物被合成并评估为潜在的三重再摄取抑制剂,用于研究结构-活性关系.最先进的化合物1-(4-(5-苯甲酰基-1H-四唑-1-基)丁基)-4-(3-苯丙基)哌嗪(2I)在体外测试中能够抑制单胺神经递质的再摄取(对于5-Ht,Ic50 = 158.7Nm,对于ne,Ic50 = 99Nm,对于da,Ic50 = 97.5Nm).
DOI:10.1016/j.Bmc.2017.02.051

专利信息

专利号:US-7645754-B2
优先权日:2001-12-20
标题 :Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use
发明人：CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO
权利人:OSI PHARM INC
摘要:The subject invention provides compounds having the structure: n n n n n n n n n n n n wherein,n R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(â•?O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(â•?O)NR 8 R 9 , —(CH 2 ) m C(â•?O)OR 10 , —(CH 2 ) k C(â•?O)NR 11 R 12 ;n wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3,n nor a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a sbject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

专利号:CA-2795762-C
优先权日:2010-04-08
标 题:Synthesis of 18f-labeled tracers in hydrous organic solvents