1310406-77-9Relevant academic research and scientific papers
Process Development and Good Manufacturing Practice Production of a Tyrosinase Inhibitor via Titanium-Mediated Coupling between Unprotected Resorcinols and Ketones
Gerfaud, Thibaud,Martin, Cédric,Bouquet, Karinne,Talano, Sandrine,Millois-Barbuis, Corinne,Musicki, Branislav,Boiteau, Jean-Guy,Cardinaud, Isabelle
, p. 631 - 640 (2017/04/28)
A concise and economically attractive process for the synthesis of a novel tyrosinase inhibitor has been developed and implemented on a multikilogram scale under GMP. A major achievement to the success of the process is the development of a direct coupling between free resorcinol and ketone. First developed under basic conditions, this coupling has been turned to a novel titanium(IV) mediated process allowing good selectivity, easy isolation, and high atom efficiency. Other key steps feature an alkene reduction by palladium catalyzed transfer hydrogenation and a urea formation using N,N′-disuccinimidyl carbonate as the carbonyl source. This route allowed us to produce kilogram batches of the candidate to support preclinical and clinical studies.
4-piperidin-4-yl-benzene -1,3-diol and synthesis of the salt, and new compd. tert-butyl 4 - (2,4-dihydroxy-phenyl) - 4-hydroxy-piperidin-1-hydroxyphenylalkanecarboxylate
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Paragraph 0078, (2017/02/28)
A method is described for the synthesis of 4-piperidin-4-yl-benzene-1,3-diol of the following formula (I): and the pharmaceutically acceptable salts thereof. Also described, is tert-butyl 4-(2,4-dihydroxy-phenyl)-4-hydroxy-piperidine-1-carboxylate as a no
METHOD FOR THE SYNTHESISING 4-PIPERIDIN-4-YL-BENZENE-1,3-DIOL AND THE SALTS OF SAME AND NOVEL COMPOUND TERT-BUTYL 4-(2,4-DIHYDROXY-PHENYL)-4-HYDROXY-PIPERIDINE-1-CARBOXYLATE
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, (2016/01/21)
A method is described for the synthesis of 4-piperidin-4-yl-benzene-1,3-diol of the following formula (I): and the pharmaceutically acceptable salts thereof. Also described, is tert-butyl 4-(2,4-dihydroxy-phenyl)-4-hydroxy-piperidine-1-carboxylate as a no
4- (AZACYCLOALKYL) -BENZENE-1, 3 -DIOL DERIVATIVES AS TYROSINASE INHIBITORS AND THEIR SYNTHESIS AND USE THEREOF
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, (2011/06/26)
The present invention concerns novel 4-(azacycloalkyl)-benzene-1,3-diol compounds with the following general formula (I): to compositions containing them, to a process for their preparation and to their use in pharmaceutical or cosmetic compositions for t
