CAS: 115314-17-5; (R)-Oxiran-2-Ylmethyl 3-Nitrobenzenesulfonate

相似化合物

115314-14-2 118712-60-0 113826-06-5

上下游产品

3-nitrobenzenesulphonyl chloride (S)-oxiranemethanol (R)-oxiranemethanol (S)-3-chloropropan-1,2-diol (2R)-(+)-N-(2,3-epoxypropyl)morpholine 4-{4-[(2R)-oxiran-2-ylmethoxy]-1,2,5-thiadiazol-3-yl}morpholine 1-O-oleyl-sn-glycerol 3-O-m-nitrobenzenesulfonate 3-O-oleyl-sn-glycerol 1-O-m-nitrobenzenesulfonate

(S)-3-氯-1,2-丙二醇,3-硝基苯磺酰氯置于potassium Phosphate,三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 5.0H,以72%的收率获得(R)-(+)-间硝基苯磺酸缩水甘油酯
参考文献:Synthesis Of 5-Oxyquinoline Derivatives For Reversal Of Multidrug Resistance
标题:Synthesis Of 5-Oxyquinoline Derivatives For Reversal Of Multidrug Resistance
摘要:Abc(atp结合盒)转运蛋白的抑制被认为是逆转多药耐药的有力工具.发现了一种具有二氟环丙基环戊二苯亚基结构的佐苏奎达,它被发现是p-糖蛋白的抑制剂,后者是研究最充分的多药外流泵之一.已合成了十二种5-氧异喹啉衍生物,它们是佐苏奎达的类似物,其中二苯亚基-哌嗪结构被二芳胺哌啶或哌啶酮衍生的缩醛或硫缩醛基团替代,这些衍生物均为纯对映异构体.它们的抑制力已经针对细菌多药耐药abc转运蛋白lmrcd和真菌pdr5进行了评估.新合成的四种化合物中有四种比佐苏奎达更有效地降低了转运活性,在lmrcd的情况下高达四倍,对于pdr5则提高了约两倍.
Doi:10.3762/bjoc.8.193

专利信息

专利号:US-10556913-B2
优先权日:2015-07-21
标 题:Asymmetric process for the preparation of thieno-indoles derivatives
发明人：BERIA ITALO; CARUSO MICHELE; DONATI DANIELE; ORSINI PAOLO
权利人:NERVIANO MEDICAL SCIENCES SRL
摘要:The present invention relates to a new process for the preparation of thieno-indole derivatives of formula (Ia) or (Ib), exploiting an asymmetric synthesis for the preparation of key (8S) or (8R) 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates, and to useful intermediate compounds of such process. n Thieno-indole derivatives are described and claimed in GB2344818, WO2013/149948 and WO2013/149946, which also disclose processes for their preparation. n Thieno-indole enantiopure derivatives can now be advantageously prepared through a new asymmetric synthesis of the key 8-(halomethyl)-7,8-dihydro-6H-thieno[3,2-e]indol intermediates, which, avoiding the chiral resolution step, provides benefits in terms of reducing time and costs of the whole process for their preparation. The synthesis starts from the N-alkylation of 5-amino-4-halo-3-alkyl-1-benzothiophene-7-ol derivatives with enantiopure glycidyl 3-nosylate, followed by intramolecular 6-endo-tet cyclization using alkyl Grignard reagents; Mitsunobu activation of the secondary alcohol promotes internal spirocyclization, affording the 4,4a,5,6-tetrahydro-8H-cyclopropa[c]thieno[3,2-e]indol-8-one derivatives; finally, stereo-electronically controlled regioselective cyclopropane opening yields the key enantiopure 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates; which can be further derivatized following teachings disclosed in WO2013/149948 or WO2013/149946, to prepare the final thieno-indole derivatives of formula (Ia) or (Ib). n Such compounds are disclosed to be alkylating compounds with cytotoxic activity, therefore useful as such in the treatment of a variety of cancers and in cell proliferative disorders, or, conjugated with different types of nucleophiles, in the preparation of Antibody Drug Conjugated derivatives.

专利号:US-7038062-B2
优先权日:2004-07-01
标题:Synthesis of cyclic trithiocarbonates from epoxides
发明人：PARKER DANE KENTON
权利人:GOODYEAR TIRE & RUBBER
摘要:This invention provides a low cost technique for synthesizing cyclic trithiocarbonates by a simple one step process from epoxides that can be conducted under atmospheric pressure. This synthesis can be depicted as follows: n nwherein R represents a moiety selected from the group consisting of alkyl groups and aryl groups, wherein R′ represents a moiety selected from the group consisting of alkyl groups, aryl groups, and hydrogen atoms, and wherein R″ represents a moiety selected from the group consisting of alkyl groups, aryl groups, and hydrogen atoms, wherein the R moiety and the R′ moiety can be bonded together to form a cyclic structure, with the proviso that R″ represents a hydrogen atom if R′ represents an alkyl group or an aryl group. In this process carbon disulfide and a thiocyanate salt, such as potassium thiocyanate, are reacted with the epoxide in an ionic liquid, such as 1-butyl-3-methylimidazolium hexafluorophosphate ([Bmim] PF 6 ) in the presence of water to produce the cyclic trithiocarbonate.

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-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-2024383853-A1
优先权日:2021-09-28
标题:Oximes and their use in treatment of gba-related diseases
发明人：NEVE SØREN; BROWN WILLIAM DALBY; THIRSTRUP KENNETH
权利人:ZEVRA DENMARK AS
摘要:The present invention relates to oximes, their synthesis, and their use for increasing GBA activity and/or levels as well as treatment of GBA-related diseases, such as Parkinson's disease.