One-pot synthesis of useful heterocycles in medicinal chemistry using a cascade strategy

Copper Pincer Complexes as Advantageous Catalysts for the Heteroannulation of ortho‐Halophenols and Alkynes

“…2‐(3,5‐Dimethoxyphenyl)benzofuran (3g): 30 Yield: 79%; pale yellow powder; mp 48–51 °C; 1 H NMR (300 Hz, CDCl 3 ): δ =7.61 (d, J= 7.1 Hz, 1 H), 7.56 (d, J= 8.7 Hz, 1 H), 7.33 (dt, J= 7.3, 1.3 Hz, 1 H), 7.29–7.25 (m, 1 H), 7.07 (d, J= 2.3 Hz, 2 H), 7.04 (s, 1 H), 6.52 (t, J= 2.3 Hz, 1 H), 3.91 (s, 6 H); 13 C NMR (75.4 MHz, CDCl 3 ): δ =161.1, 155.7, 154.9, 132.3, 129.1, 124.4, 123.0, 121.0, 111.2, 103.1, 101.9, 101.1, 55.5; IR (film): ν =2958, 2836, 1599, 1450, 1333 cm −1 ; MS: m / z (%)=255 (M + , 100), 254 (36); HR‐MS: m/z =255.1034, calcd. for C 16 H 15 O 3 : 255.1021.…”

Pyrazine-2(1H)-thione

“…As a result, pyrazine has weaker basic properties than pyridine, pyridazine and pyrimidine. Pyrazine derivatives play an important role in chemotherapy (Wu et al, 2012;Polshettiwar & Varma 2008;Goya et al, 1997). Its derivatives possess diverse biological activities such as antidiabetic, diuretic (Pranab et al, 2011), antiinflammatory (Chandrakant & Naresh, 2004), antimicrobial (Mallesha & Mohana 2011), analgesic (Dolez ˇal et al, 2007) and anticancer (Kayagil & Demirayak, 2011).…”

Synthesis of 6-Substituted 3-(Alkoxycarbonyl)-5-aryl-α-pyrones

“…Benzyl ethyl ketone derivatives 7b-f containing such substituents as F, CF 3 , NO 2 , OMe, and Ph at the para position of the benzene ring were prepared by Negishi coupling. 14 In the cases of aryl benzyl ketone derivatives 12 and 13, the Claisen decarboxylation reaction 15 was employed. With the Claisen decarboxylation reaction, thiophene-2-acetic acid (14) could be also converted into the corresponding ketone derivative 15.…”