122742-14-7Relevant articles and documents
Method for efficiently preparing azaindole CRTH2 receptor antagonist intermediate
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Paragraph 0048-0049; 0052-0053, (2020/10/21)
The invention provides a method for preparing an azaindole compound shown as a formula (I). The method comprises the following steps: carrying out simple conversion on an initial raw material D-pyroglutamic acid to obtain an intermediate shown as a formula (II); carrying out ring opening on the intermediate shown as the formula (II) by 2-(N-tert-butyloxycarbonylamino)-3-methylpyridine under the action of organic alkali; and adding organic acid to directly obtain an azaindole compound shown as a formula (III), protecting secondary amine, activating hydroxyl or performing Mitsunobu reaction, andperforming ring closing to obtain the formula (I). According to the method provided by the invention, D-pyroglutamic acid is used as a starting material, so that complex processes such as chiral auxiliary synthesis, chiral resolution or introduction of chiral amino by enzyme catalytic reaction are avoided; therefore, the synthesis steps are greatly shortened, the cost is greatly reduced, and themethod is suitable for industrial large-scale production.
Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1 826
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, (2011/05/03)
A compound of formula (I): and pharmaceutically-acceptable salts thereof, wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described
Renin Inhibitors Containing Conformationally Restricted P1-P1' Dipeptide Mimetics
Williams, Peter D.,Perlow, Debra S.,Payne, Linda S.,Holloway, M. Katharine,Siegl, Peter K. S.,et al.
, p. 887 - 900 (2007/10/02)
A series of renin inhibitors containing lactam-bridged P1-P1' dipeptide mimetics based on the ACHPA (4(S)-amino-5-cyclohexyl-3(S)-hydroxypentanoic acid) design was studied.The inhibitors were obtained by aldol addition of various lac
