专利号:US-6087512-A 优先权日:1996-09-18 标题:Process for preparation of glycidyl ether 发明人:FURUKAWA YOSHIRO; KITAORI KAZUHIRO; YANAGIMOTO TETSUYA; MIKAMI MASAFUMI; YOSHIMOTO HIROSHI; OTERA JUNZO 权利人:DAISO CO LTD 摘要:A process for preparation of a glycidyl ether which is characrelized in reacting an epoxy compound of the formula ##STR1## wherein X is halogen or sulfonyloxy in the presence of a fluoride salt, with an alcohol. According to the above method, glycigyl ethers or their optically active compounds important as intermediates for synthesis of medicines are easily obtained in good yield and especially the optically active compounds are obtained with highly optical purity.
专利号:US-6057476-A 优先权日:1996-09-18 标题:Process for the preparation of 3-amino-2-hydroxy-1-propyl ethers 发明人:FURUKAWA YOSHIRO; KITAORI KAZUHIRO; MIKAMI MASAFUMI; YOSHIMOTO HIROSHI; OTERA JUNZO 权利人:DAISO CO LTD 摘要:A process for preparation of 3-amino-2-hydroxy-1-propyl ether of the formula ##STR1## wherein R 1 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic ring, R 2 and R 3 are the same or different hydrogen atom, a substituted or unsubstituted alkyl, or may form a ring together with an adjacent nitrogen atom, which ring may be interrupted with nitrogen atom, oxygen atom or sulfur atom, n which is characterized in reacting an epoxy compound of the formula ##STR2## wherein X is halogen, in the presence of a fluoride salt, with an alcohol and then reacting an amine. n According to the above method, an intermediates for synthesis of medicines is obtained in good yield and highly optical purity.
专利号:US-11434195-B2 优先权日:2017-07-20 标题:Compositions and methods for treatment of central nervous system tumors 发明人:SVETLOV STANISLAV IGOREVICH 权利人:UNIV FLORIDA 摘要:Compounds, pharmaceutical compositions, and methods for treating cancer, in particular brain cancer, are provided, including amphiphilic fatty acid/alcohol ethers (AIPs) comprising endocannabinoid and FABP motifs covalently linked to a beta-adrenoreceptor antagonist motif in one molecule. The invention includes methods for inhibiting growth of brain cancer cells by contacting the compound(s) with brain cancer cells. The invention provides a method for treating both brain cancer and brain cancer metastases, and for suppression of regrowth of brain cancer cells after radiation, surgical treatment, or chemotherapy of brain cancer. The invention also comprises an optimized chemical synthesis of the AIP compounds and methods of using the compounds, alone or in combination with another agent, for suppressing the growth of brain cancer cells, and enhancing survival of normal CNS cells, or improving recuperation from radiation, surgical or chemotherapy.
专利号:US-5274160-A 优先权日:1991-08-22 标 题:Method and apparatus for synthesis of highly isomerically pure stereoisomers of glycidol derivatives 发明人:HAHN ROGER C 权利人:UNIV SYRACUSE 摘要:There is disclosed a process for producing an alkyl casylate by the reaction of a metal casylate or an enantiomer of a quaternary casylate with a trialkyl phosphite in the presence of a slight molar excess of sulfuric acid. According to one aspect of the invention the reaction is conducted under heat in the presence of concentrated sulfuric acid. When the reaction is complete, an organic layer that contains the alkyl casylate is isolated. In another aspect of the invention at least 1.0 equivalents of a trialkyl phosphite is added to a thoroughly dried enantiomer of camphorsulfonic acid, and the mixture optionally heated to about 80° C. The reaction is allowed to proceed until camphorsulfonic acid is no longer present. Thereafter all phosphorus-containing species are selectively removed by distillation at reduced pressure to obtain a pure alkyl casylate in high yield.
专利号:US-2009247618-A1 优先权日:2008-03-26 标题 :Process for preparation of benzo-fused heteroaryl derivatives 发明人:BALLENTINE SCOTT A; REANY LAURA 权利人:BALLENTINE SCOTT A; REANY LAURA 摘要:The present invention is directed to processes for the preparation of benzo-fused heteroaryl derivatives, useful for the treatment of epilepsy and related disorders. The present invention is further directed to processes for the preparation of intermediates in the synthesis of the benzo-fused heteroaryl derivatives.
专利号:US-2006111438-A1 优先权日:2004-10-21 标 题:Asymmetric synthesis of substituted dihydrobenzofurans 发明人:GONTCHAROV ALEXANDER V; KHAFIZOVA GULNAZ; POTOSKI JOHN R; YU QING; SHAW CHIA-CHENG; STACK GARY P; ZHOU DAHUI 权利人:WYETH CORP 摘要:The present invention concerns production of a compound of the formula n n nor a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula: n n nwhere Ar, Y, R 1 , R y , R 2 , and m are as defined herein.