乙酸苯酯置于盐酸,三乙基硅烷,Aluminum (III) Chloride,Sodium Tetrahydroborate,Sodium Methylate,Caesium Carbonate,三乙胺,三氟乙酸,Sodium Iodide体系中,用 四氢呋喃,甲醇,二氯甲烷,水,二甲基亚砜,1,2-二氯乙烷 用作溶剂,化学反应 12.5H,反应生成盐酸芬戈莫德 参考文献:Preparation Of Fingolimod And Its Salts 标题:Preparation Of Fingolimod And Its Salts 摘要:本申请提供了制备非格列酮及其药用可接受盐的过程,非格列酮盐酸盐的纯化过程以及非晶态非格列酮盐酸盐的制备过程.
专利号:US-10865163-B2 优先权日:2017-12-20 标题:Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds 发明人:YOUNG MICHAEL C; KAPOOR MOHIT 权利人:UNIV TOLEDO 摘要:Methods of synthesizing compounds using CO 2 as a directing group for C—H functionalization, and compounds made thereby, are described.
专利号:US-11999693-B2 优先权日:2015-09-24 标 题:Synthetic sphingolipid-like molecules, drugs, methods of their synthesis and methods of treatment 发明人:EDINGER AIMEE L; HANESSIAN STEPHEN 权利人:UNIV CALIFORNIA; THE UNIV DE MONTREAL 摘要:Small molecules comprised of azacyclic constrained sphingolipid-like compounds and methods of their synthesis are provided. Formulations and medicaments are also provided that are directed to the treatment of disease, such as, for example, neoplasms, cancers, and other diseases. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.
专利号:US-2019185392-A1 优先权日:2017-12-20 标 题 :Carbon Dioxide as a Directing Group for C-H Functionalization Reactions Involving Lewis Basic Amines, Alcohols, Thiols, and Phosphines for the Synthesis of Compounds
专利号:US-9815772-B2 优先权日:2013-03-05 标题:Process for the preparation of 2-amino-1,3-propane diol compounds and salts thereof 发明人:KUMAR KOTHAKONDA KIRAN; ASWATHANARAYANAPPA CHANDRASHEKAR; CHANDREGOWDA DHARSHAN JAKKALI; DUVVA CHANDRASEKHAR; PULLELA VENKATA SRINIVAS 权利人:BIOCON LTD 摘要:The present disclosure relates to processes for the preparation of 2-amino-1,3-propane diol compounds and their hydrochloride salts. Particularly, the present disclosure relates to processes for synthesizing 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol and its hydrochloride salt 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride respectively. The said process is safe, commercially feasible for large-scale synthesis and has improved efficacy along with many other advantages. The present disclosure also relates to the novel polymorphs of 2-amino-1,3-propane diol compound and its hydrochloride salt, where in 2-amino-1,3-propane diol compound is 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol, and its hydrochloride salt is 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride.
专利号:EP-2502901-A4 优先权日:2011-01-25 标 题 :NEW METHOD FOR SYNTHESIS OF FINGOLIMOD HYDROCHLORIDE
专利号:US-2023047961-A1 优先权日:2019-12-03 标 题 :The cholesterol-syntesis intermediates for treatment demyelinating disorders 发明人:BERGHOFF STEFAN; SAHER GESINE 权利人:MAX PLANCK GESELLSCHAFT 摘要:The present invention relates to a cholesterol-synthesis intermediate as pharmaceutically active agent and/or pharmaceutical composition comprising the cholesterol-synthesis intermediate optionally together with one or two further pharmaceutically active agent(s) for use in the prophylaxis and/or treatment of demyelinating disorders/diseases, in particular multiple sclerosis.
参考文献:10.1038/nrneurol.2011.105 摘要:Hohlfeld R. Multiple sclerosis: Cladribine--a contentious therapeutic contender for MS. Nat Rev Neurol. 2011 Jul 12;7(8):425–7. doi: 10.1038/nrneurol.2011.105. 摘要:Fingolimod. Prescrire Int. 2011 Jul;20(118):173–4, 176. 参考文献:10.1007/s00115-011-3262-2 摘要:Zipp F, Gold R. [Neuroprotection in the treatment of multiple sclerosis]. Nervenarzt. 2011 Aug;82(8):973–7. doi: 10.1007/s00115-011-3262-2. 参考文献:10.1182/blood-2011-01-331447 摘要:Liao A, Broeg K, Fox T, Tan SF, Watters R, Shah MV, Zhang LQ, Li Y, Ryland L, Yang J, Aliaga C, Dewey A, Rogers A, Loughran K, Hirsch L, Jarbadan NR, Baab KT, Liao J, Wang HG, Kester M, Desai D, Amin S, Loughran TP, Liu X. Therapeutic efficacy of FTY720 in a rat model of NK-cell leukemia. Blood. 2011 Sep 08;118(10):2793–800. 参考文献:10.1158/1078-0432.ccr-05-0447 摘要:Lee TK, Man K, Ho JW, Wang XH, Poon RT, Xu Y, Ng KT, Chu AC, Sun CK, Ng IO, Sun HC, Tang ZY, Xu R, Fan ST. FTY720: a promising agent for treatment of metastatic hepatocellular carcinoma. Clin Cancer Res. 2005 Dec 01;11(23):8458–66. doi: 10.1158/1078-0432.ccr-05-0447.