4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase

Enantioselective LaIII‐pyBOX‐Catalyzed Nitro‐Michael Addition to (E)‐2‐Azachalcones

“…(S)-2-Amino-3-(naphthalen-1-yl)propan-1-ol (4a): [24] To a solution of l-3-(naphthalen-1-yl)alanine (3a, 1.5 g, 7.0 mmol) in anhydrous THF (15 mL) was added dropwise BH 3 ·Me 2 S (2 m in THF, 8.7 mL, 17.4 mmol) under nitrogen. The reaction mixture was then introduced in a bath at 60°C and stirred overnight.…”

Synthesis of New Derivatives of 4‐(4,7,7‐Trimethyl‐7,8‐dihydro‐6H‐benzo[b]pyrimido[5,4‐e][1,4]thiazin‐2‐yl)morpholine

“…Our previous published study on the synthesis and using of 5-amino-6-methyl-2-morpholinopyrimidine-4-thiol (1) [26] in a typical heterocyclization reaction prompted us to explore another aspects of treatment with the synthesized 2-bromo-5,5-dimethylcyclohexane-1,3-dione (2) [27] through which obtained the corresponding fused 4,7,7-trimethyl-2-morpholino-7,8-dihydro-5H-benzo[b]pyrimido [5,4-e] [1,4] thiazin-9(6H)-one (3) in the presence of Et 3 N at room temperature (Scheme 1).…”

Efficient Synthesis of N‐Substituted 2,4‐Azepandione Ring System as an Active Intermediate for Heterocyclic Syntheses

“…), and their analogues, which were recently identified in a screen for compounds that arrest cells in mitosis . Also, it represents the consecutive building of the bicyclic oxazolo[4,5‐ c ]azepine or thiazolo[4,5‐ c ]azepine ring systems , which act as a selective inhibitor of phosphoinositide 3‐kinase . Drazepinone is a potential natural herbicide and the new diacetylenic natural products; montiporyne A–F compounds exhibit bioactivity against certain solid tumor cells .…”