613-70-7Relevant articles and documents
Synthesis of a TNF inhibitor, flurbiprofen and an: I -Pr analogue in enantioenriched forms by copper-catalyzed propargylic substitution with Grignard reagents
Isogawa, Yukari,Kobayashi, Yuichi,Ogawa, Narihito,Takashima, Yuji,Tsuboi, Atsuki
supporting information, p. 9906 - 9909 (2021/12/07)
The copper-catalyzed substitution reaction of diethyl phosphate derived from TMSCCCH(OH)CH2CH2OTBDPS with 3-c-C5H9-4-MeOC6H3MgBr, followed by several transformations, afforded a tumor necrosis factor inhibitor possessing a Ph-acetylene moiety. The inhibitor was also synthesized from phenylacetylene phosphate PhCCCH(OP(O)(OEt)2)CH2CH2OTBDPS. Furthermore, the substitution of phosphates derived from TMSCCCH(OH)CH3 and TMSCCCH(OH)-i-Pr with 3-F-4-PhC6H3MgBr gave the corresponding substitution products, which were transformed to flurbiprofen and its i-Pr analogue, respectively. The copper-catalyzed substitutions in these syntheses proceeded in a regio- and stereoselective manner. This journal is
Methods for preparation of apremilast
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Page/Page column 20-21, (2021/05/19)
The present invention discloses a method for preparation of Apremilast. β-phthalimino vinylsulfones are reacted through the asymmetric addition reaction to form an addition product, and the drug of Apremilast can be obtained from the addition product through simple reactions. The method is a process for synthesizing Apremilast in a more efficient way.
Preparation method of plant growth regulation compound sodium nitrophenolate
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Paragraph 0025-0087, (2021/08/06)
The invention relates to the field of preparation of agricultural auxiliaries, in particular to a preparation method of plant growth regulation compound sodium nitrophenolate. According to the invention, acetyl chloride is adopted to replace acetic anhydride which is a precursor to serve as a protecting group for hydroxyl acetylation, so that the acquisition difficulty of process raw materials is reduced, and the production cost of 5-nitroguaiacol sodium salt is controlled; and besides, a phase transfer catalyst is applied to the hydrolysis reaction of 5-nitroacetyl guaiacol, so that the hydrolysis of the product can be effectively promoted, the yield of the hydrolysis reaction is greatly improved, and the overall yield of the 5-nitroguaiacol sodium salt is further improved. The prepared 5-nitroguaiacol sodium salt has the advantage of low cost, and as a main effective component of the compound sodium nitrophenolate, the 5-nitroguaiacol sodium salt can improve the market competitiveness of the compound sodium nitrophenolate product, avoid the behavior that the drug effect of the compound sodium nitrophenolate product is reduced due to the fact that the cost of the 5-nitroguaiacol sodium salt is high and the ratio is reduced by bad manufacturers, and make contribution for promoting the benign development of the market.