535-17-1Relevant articles and documents
Monnin
, p. 892,893 (1961)
Ni-Catalyzed C(sp3)–O Arylation of α-Hydroxy Esters
Monteith, John J.,Rousseaux, Sophie A. L.
supporting information, p. 9485 - 9489 (2021/12/09)
A Negishi cross-coupling of α-hydroxy ester derivatives and arylzinc reagents has been developed. This reaction tolerates both primary and secondary C(sp3)–O alcohol precursors and achieves efficient cross-coupling under Ni catalysis without the need for added external metal reductant, photocatalyst, or additives. The arylation of readily accessible C(sp3)–O electrophiles in this operationally simple, rapid, and mild reaction provides a complementary way of accessing desirable α-aryl ester products.
NOVEL STING AGONISTS
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Paragraph 0756; 0761; 0763, (2020/05/14)
The present invention provides compounds of Formula I′: wherein , W, X, Y, Z, Z1, Z2, R1, R2, R3, R4 and R5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.
Industrial preparation method of aclatonium napadisilate
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Paragraph 0031-0044; 0047-0050, (2019/11/13)
The invention discloses an industrial preparation method of aclatonium napadisilate. The industrial preparation method comprises the following steps that lactic acid reacts with acetic anhydride, chloroformate and N,N-dimethylethanolamine in sequence to obtain acetyllactylcholine, acetyllactylcholine is added with acid to be prepared into a salt and then separated, and a product reacts with 1,5-naphthalenedisulfonic acid dimethyl ester to obtain aclatonium napadisilate. The industrial preparation method has the advantages that aclatonium napadisilate is prepared by a ''mixed acid anhydride strategy'', and the use of a volatile highly corrosive reagent can be avoided; water can be used as a solvent for preparation of an intermediate, and the amount of an organic solvent can be avoided or reduced; a ''one-pot method'' can be adopted to prepare the intermediate to reduce unit operation; the solvent can be directly added for crystallization in the post-processing process of the preparationof a finished product to improve the purity of the product; and the reaction scale can be enlarged to more than ten kilograms.
