15567-95-0Relevant articles and documents
Hydrolysis of iminium ethers derived from the reaction of ketones with hydroxy azides: Synthesis of macrocyclic lactams and lactones
Forsee, Jennifer E.,Aube, Jeffrey
, p. 4381 - 4385 (1999)
The hydrolysis of iminium ether intermediates formed by a nitrogen insertion sequence involving azido alcohols 1 or 2 and ketones was investigated. Ketones containing 6-12-membered rings were surveyed and shown to provide lactams and lactones in good to excellent overall yield. Reactions employing acetone or 5-nonanone gave similar results, generating analogous amides and esters. The relative amounts of lactone vs lactam produced in a given reaction were found to depend on the structures of the reactants and the pH of the basic media used to hydrolyze the iminium ethers. A mechanism accounting for the formation of each product is discussed in terms of ring strain and the protonation state of ortho ester aminal intermediates.
Cycloalkyl and heterocycloalkyl inhibitors as well as preparation method and application thereof
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Paragraph 0367-0370, (2021/04/26)
The invention relates to cycloalkyl and heterocycloalkyl inhibitors as well as a preparation method and application thereof. Specifically, the compounds disclosed by the invention have a structure as shown in a formula (I). The invention also discloses a preparation method of the compounds and application of the compounds as KRASG12C inhibitors. The compounds have a good selective inhibition effect on KRASG12C, and have better pharmacodynamic and pharmacokinetic properties and lower toxic and side effects.
Reactions on a Solid Surface. A Simple, Economical, and Efficient Acylation of Alcohols, Amines over Al2O3
Yadav, Veejendra K.,Babu, K. Ganesh
, p. 577 - 580 (2007/10/03)
Al2O3 brings about a rapid acylation of a range of alcohols and amines with acid chlorides and acid anhydrides, respectively. Amines are easily Boc- and Cbz-protected on reaction with Boc-anhydride and Cbz-Cl, respectively. The acylation of phenols is slow enough to allow chemoselective acylation of alcohols and amines in the presence of phenols.