CAS: 37743-18-3; 5-(Dimethylamino)-4,4-Diphenyl-3,4-Dihydro-2H-Furan-1-Ium Bromide

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CAS号124-40-3 二甲胺 | CAS号37742-98-6 4-溴-2,2-二苯基丁酸 | CAS号497-19-8 纯碱 | CAS号956-89-8 α,α-二苯基-γ-丁内酯 | CAS号34552-83-5 盐酸洛哌丁胺 | CAS号53179-11-6 洛哌丁胺 | CAS号53179-10-5 Fluperamide

📜α,α-二苯基-γ-丁内酯置于氯化亚砜,氢溴酸,Sodium Carbonate,溶剂黄146体系中,用 氯仿,水,甲苯 用作溶剂,化学反应 52.0H,反应生成3,3-二苯基四氢呋喃-2-亚基二甲基溴化胺
参考文献:A High-Yield Route To Synthesize The P-Glycoprotein Radioligand [ C]N-Desmethyl-Loperamide And Its Parent Radioligand [ C]Loperamide
标题:A High-Yield Route To Synthesize The P-Glycoprotein Radioligand [ C]N-Desmethyl-Loperamide And Its Parent Radioligand [ C]Loperamide
摘要:N-Desmethyl-Loperamide And Loperamide Were Synthesized From A,A-Diphenyl-C-Butyrolactone And 4-(4-Chlorophenyl)-4-Hydroxypiperidine In Five And Four Steps With 8% And 16% Overall Yield,Respectively. The Amide Precursor Was Synthesized From 4-Bromo-2,2-Diphenylbutyronitrile And 4-(4-Chlorophenyl)-4-Hydroxypiperidine In 2 Steps With 21-57% Overall Yield. [c-11] N-Desmethyl-Loperamide And [c-11] Loperamide Were Prepared From Their Corresponding Amide Precursor And N-Desmethyl-Loperamide With [c-11] Ch3Otf Through N-[c-11] Methylation And Isolated By HPLC Combined With Solid-Phase Extraction (Spe) In 20-30% And 10-15% Radiochemical Yields,Respectively,Based On [c-11] Co2 And Decay Corrected To End Of Bombardment (Eob),With 370-740 Gbq/lmol Specific Activity At Eob. (C) 2013 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2013.08.024

专利信息

专利号:US-3714159-A
优先权日:1971-03-30
标 题:2,2-diaryl-4-(4'-aryl-4'-hydroxy-piper-idino)-butyramides
发明人：JANSSEN P; NIEMEGEERS C; STOKBROEKX R; VANDENBERK J
权利人:JANSSEN PHARMACEUTICA NV
摘要:COMPOUNDS OF THE CLASS OF 2,2-DIARYL-4-(4''-ARYL-4''HYDROXY-PIPERIDINO)BUTYRAMIDES WHEREIN SAID ARYL AND SAID AMIDE FUNCTIONS ARE VARIOUSLY DEFINED GROUPS, SAID BUTURAMIDES HAVING ANTI-DIARRHEAL AND ANALGESIC ACTVITES; ALSO INCLUDED ARE NOVEL INTERMEDIATES USED IN THE SYNTHESIS OF SAID BUTYRAMIDES.