CAS: 4205-90-7; N-(2,6-Dichlorophenyl)-4,5-Dihydro-1H-Imidazol-2-Amine

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CAS号57647-79-7 苯可乐定 | CAS号87-69-4 酒石酸 | CAS号141-43-5 2-氨基乙醇 | CAS号111225-65-1 amino-(2,6-dich... | CAS号107-15-3 乙二胺 | CAS号33178-86-8 烯丙尼定

📜盐酸可乐定置于sodium Hydroxide体系中,用 水 作为反应溶剂,以94%的收率获得产物可乐定
参考文献:可乐定的分子结构:气相电子衍射,单晶x射线衍射和量子化学研究†
标题:可乐定的分子结构:气相电子衍射,单晶x射线衍射和量子化学研究†
摘要:这项研究提出了使用气相电子衍射(ged)首次确定气相中降压药可乐定的分子结构.精细化得到了量子化学计算(qc)的支持.从理论上研究了互变异构和构象分布,为气相中单一构象异构体的存在提供了解释.已显示可乐定的分子构象具有近似垂直的苯基和咪唑烷环排列,如扭转角c2-N6-C7-C8 =-72(6)°所述.下述结构参数(以埃键长和键角以度与3中得到σ在括号中):-[r(c Hh-C Hh)= 1.549(7),R(c Hh-n H)av = 1.470(7),R(n H-c)av = 1.388(2),R(c N)= 1.286(7),R(cn)= 1.388(2)),R(cc)av = 1.403(2),R(cc)av = 1.737(2); ∠(n H-c-n H)= 108.1(11),H(c Hh-n H-c)av = 109.7(12),∠(c Hh-c Hh-n
DOI:10.1039/c6Cp08401J

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-6271379-B1
优先权日:2000-03-08
标题:Intermediates useful for the synthesis of huperzine A
发明人：TUECKMANTEL WERNER; KOZIKOWSKI ALAN P
权利人:UNIV GEORGETOWN
摘要:Intermediates useful for the synthesis of huperzine A represented by the structures below, n and methods for their synthesis, wherein: n R 1 is lower alkyl, benzyl, or substituted benzyl; n X is a suitable leaving group; n Y is an electron withdrawing group that can subsequently be converted into an amino group; n one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-12264143-B2
优先权日:2020-12-17
标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use
发明人：SAMMIS GLENN M; ROGGEN MARKUS
权利人:NALU BIO INC
摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.

专利号:US-11459303-B2
优先权日:2019-06-21
标题 :Process for the synthesis of lofexidine
发明人：DONNOLA MONICA; BAROZZA ALESSANDRO; ROLETTO JACOPO; PAISSONI PAOLO
权利人:PROCOS SPA
摘要:Disclosed is a process for the synthesis of lofexidine of formula (I) and the hydrochloride salt thereof (II), from ethyl 2-(2,6-dichlorophenoxy)propionate (III) and ethylenediamine in the presence of tetravalent titanium alkoxides, preferably titanium isopropoxide, in an apolar solvent such as toluene. A further object of the present invention is a process for the preparation of the intermediate ethyl 2-(2,6-dichlorophenoxy)propionate (III) from 2,6-dichlorophenol and ethyl 2-chloropropionate in the presence of a polar aprotic solvent and an alkali or alkaline earth carbonate salt, preferably potassium carbonate. Both processes are more cost-effective and more easily industrially scalable than the known procedures, thus enabling the active ingredient to be obtained with high yields at a limited cost.