Benzo[c][2,7]naphthyridines as inhibitors of PDK-1

Dialkylbiaryl phosphines in Pd-catalyzed amination: a user's guide

“…A number of examples of the coupling of anilines using dialkylbiaryl phosphines in the synthesis of pharmaceuticals have appeared. 6, 120, 122, 197, 203 Catalysts based on L1 are the most active for the arylation of these substrates and provide excellent selectivity for mono-:diarylated products (ie. for formation of diarylamine rather than triarylamine).…”

An efficient three-component, one-pot synthesis of 2-alkylthio-4-amino-5-cyano-6-aryl(alkyl)pyrimidines in water

“…The scope of this method was further investigated through the reaction of pyridine-3-carboxaldehyde and malononitrile with various S-alkylisothiouronium salts under the same reaction conditions(entries [19][20][21][22][23]. The results showed that all reactions proceeded smoothly to afford the 2-alkylthio-4-amino-5-cyano-6-(3-pyridinyl)pyrimidines in 54-74 % yield.…”

“…To demonstrate the application of 2-alkylthio-4-amino-5cyano-6-(3-pyridinyl)pyrimidines in the synthesis of pyrimidine derivatives, we have successfully constructed two [20][21][22].…”

“…The pyrimidine-fused heterocyclic compounds D and E are PDK1 inhibitors and TLR modulators, respectively ( Fig. 1) [20][21][22]. To the best of our knowledge, there are mainly two methods for the synthesis of 2-alkylthio-4-amino-5-cyano-6aryl(alkyl)pyrimidines [23][24][25][26][27][28][29], as shown in Scheme 1.…”

Green Synthesis of Fused Imidazo[1,2‐a][1,8]naphthyridine Derivatives Catalyzed by DABCO under Solvent‐Free Solid‐State Conditions and Their Biological Evaluation

“…Crystal structure of phosphoinositide‐dependent protein kinase‐1 (PDK‐1) was obtained from the protein data bank (3H9O) and imported into Discovery studio 2.5. Crystallized water molecules were removed, and polar hydrogen was added to the complex structure, and 3H9O was applied CHARM force field, and minimizations were performed until the average root mean square deviation of the non‐hydrogen atoms reached 0.3 A o .…”