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.
参考标题:Design And Synthesis Of Novel, Potent And Selective Hypoxanthine Analogs As Adenosine A 1 Receptor Antagonists And Their Biological Evaluation 作者:Summon Koul,Vidya Ramdas,Dinesh A. Barawkar,Yogesh B. Waman,Neela Prasad,Santosh Kumar Madadi,Yogesh D. Shejul,Rajesh Bonagiri,Sujay Basu,Suraj Menon,Srinivasa B. Reddy,Sandhya Chaturvedi,Srinivas Rao Chennamaneni,Gaurav Bedse,Rhishikesh Thakare,Jayasagar Gundu,Sumit Chaudhary,Siddhartha De,Ashwinkumar V. Meru,Venkata Palle,Anita Chugh,Kasim A. Mookhtiar |发布日期:2017.3 摘要:Multipronged Approach Was Used To Synthesize A Library Of Diverse C-8 Cyclopentyl Hypoxanthine Analogs From A Common Intermediate Iii. Several Potent And Selective Compounds Were Identified And Evaluated For Pharmacokinetic (Pk) Properties In Wistar Rats. One Of The Compounds 14 With Acceptable Pk Parameters Was Selected For Testing In In Vivo Primary Acute Diuresis Model. The Compound Demonstrated
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 216. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 134. 摘要:Takaya, J.; Iwasawa, N., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 282. 摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118