CAS: 2380-94-1; 4-Hydroxyindole

上下游产品

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2,6-二硝基甲苯置于raney Ni (W-2) Palladium On Activated Charcoal,磷酸,硫酸,氢气,四乙基对甲苯磺酸铵体系中,用 甲醇,邻二甲苯,N,N-二甲基甲酰胺 用作溶剂,25.0~220.0 °C,911.92 Kpa 条件下,反应 53.13H,反应生成4-羟基吲哚
参考文献:通过相应的二氢吲哚轻松合成 4-羟基和 4-氨基吲哚
标题:通过相应的二氢吲哚轻松合成 4-羟基和 4-氨基吲哚
摘要:2-(2,6-二氨基苯基)乙醇在70%磷酸水溶液中加热可转化为4-羟基二氢吲哚,在30%硫酸水溶液中加热可转化为4-氨基二氢吲哚.4-羟基-和4-氨基吲哚都是通过二氢吲哚在1,4-二甲基苯中在钯炭上回流脱氢得到的.
Doi:10.1246/bcsj.62.3742

专利信息

专利号:WO-2024062080-A1
优先权日:2022-09-21
标题:Improved synthesis of psilocybin derivatives
发明人：HAMMES CHRISTIAN; STÖCKLI STEFAN
权利人:CARBOGEN AMCIS AG; AAMANYA AG
摘要:The present invention relates to an improved synthesis of psilocybin and alkyl- derivatives of psilocybin such as ethocybin (4-phosphoryloxy-N,N-diethyltryptamine, also known as phosphoryloxy-DET, PO-DET or CEY-39) and furthermore, relates to intermediates useful in the synthesis of these compounds.

专利号:US-6306179-B1
优先权日:1997-10-22
标题:Method for the synthesis of 2-hydroxyalkyl-para-phenylenediamines, new 2-hydroxyalkyl-para-phenylenediamines, their use for oxidation dyeing, dyeing compositions and methods of dyeing
发明人：GENET ALAIN; LAGRANGE ALAIN
权利人:OREAL
摘要:The present invention relates to a new method for the synthesis of 2-hydroxyalkyl-para-phenylenediamines which are substituted or unsubstituted at the 5-position of the benzene ring, new 2-hydroxyalkyl-para-phenylenediamines which are substituted or unsubstituted at the 5-position of the benzene ring, their use for the oxidation dyeing of keratinous fibers, the dyeing compositions containing them, as well as the methods of dyeing using them.

专利号:US-4806655-A
优先权日:1986-07-03
标题:Process for the stereospecific synthesis of indole derivatives
发明人：WAGNON JEAN; PLOUZANE CLAUDE; TONNERRE BERNARD; NISATO DINO
权利人:SANOFI SA
摘要:The present invention relates to a process for the stereo-specific synthesis of indole derivatives of formula: ##STR1## which consists in using 3-tosyloxy-1,2-O-isopropylidenepropane-1,2-diol (II) in an optically pure form in order to introduce the asymetric carbon C* of compound (I). Compound (II) is condensed with a suitable primary amine in order to prepare an oxazolidinone and condensation with a suitable phenol, and the oxazolidinone ring is then opened to form an indole compound (I).

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-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.