173676-54-5Relevant articles and documents
Phosphine-Catalyzed [3+2] or [4+2] Cycloaddition/SN2 Substitution Domino Reaction of ortho-Aminotrifluoroaceto- phenone Derivatives with Hex-3-yn-2-one: Preparation of Functionalized 1-Benzazepine Compounds
Sun, Yao-Liang,Wei, Yin,Shi, Min
, p. 3176 - 3185 (2017)
In this paper, we disclose a novel strategy for the phosphine-catalyzed cycloaddition/SN2 substitution domino reaction, giving functionalized O-bridged benzoazepine and benzoxazepine derivatives in moderate to good yields. Changing the N–H protecting group of ortho-aminotrifluoroacetophenone derivatives gave different bridged-ring products in one step. (Figure presented.).
Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains
Jin, KaiJun,Sang, YaLi,Han, Sheng,De Clercq, Erik,Pannecouque, Christophe,Meng, Ge,Chen, FenEr
, p. 11 - 20 (2019/05/15)
A novel series of dihydroquinazolin-2-amine derivatives were synthesized and evaluated for their anti-HIV-1 activity in MT-4 cell cultures. All of the molecules were active against wild-type HIV-1 with EC50 values ranging from 0.61 μM to 0.84 nM. The most potent inhibitor, compound 4b, had an EC50 value of 0.84 nM against HIV-1 strain IIIB, and thus was more active than the reference drugs efavirenz and etravirine. Moreover, most of the compounds maintained high activity (low-micromolar EC50 values)against strains bearing the reverse transcriptase (RT)E138K mutation. Compound 4b had EC50 values of 3.5 nM and 66 nM against non-nucleoside reverse transcriptase inhibitor-resistant strains bearing the RT E138K and RES056 mutations. In enzyme activity assays, compound 4b exhibited an IC50 value of 10 nM against HIV-1 RT. Preliminary SARs and molecular docking studies provide valuable insights for further optimization.
Synthesis of cyclopropylacetylene
-
, (2008/06/13)
The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is a reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one which is a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
