17518-98-8Relevant articles and documents
A convergent strategy towards febrifugine and related compounds
Maiden,Mbelesi,Procopiou,Swanson,Harrity
, p. 4159 - 4169 (2018/06/12)
We report a modular five step synthetic route to the febrifugines that employs 2-(chloromethyl)allyl-trimethylsilane as a conjunctive reagent for the coupling of the piperidine and quinazolinone groups. We also demonstrate the application of a recent Rh-catalyzed quinazolinone synthesis for the facile generation of febrifugine analogs.
The drug intermediate halofuginone, fruits alkone parent nucleus synthesis method
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Paragraph 0044; 0050; 0051, (2018/11/03)
The invention discloses a drug intermediate of halofuginone and a synthesis method of a halofuginone parent nucleus. The structural formula of the intermediate is disclosed in the specification. The synthesis method of the halofuginone parent nucleus is characterized by comprising the following steps: 1) in the presence of a catalyst, heating 3-bromo-4-chloroaniline and trimethyl orthoformate to sufficiently react, cooling, sufficiently reacting with NH3, separating, and carrying out primary purification to obtain a solid crude product; and 2) in the presence of a catalyst, sufficiently heating the obtained solid, acetic acid, CO and O2 to react, separating and purifying to obtain the end product. The synthesis method is a two-step process, and has the advantages of simple technique, environment friendliness, high yield and very low cost since the raw materials are accessible 3-bromo-4-chloroaniline and trimethyl orthoformate.
INHIBITORS OF KRAS G12C
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Page/Page column 239, (2015/04/28)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.