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. 2020 Sep 14;10(24):11178–11196. doi: 10.7150/thno.42587

Scheme 1.

Scheme 1

(A) Synthesis of mGlu2 NAMs 14a-14g. Reactions and conditions: (i) POCl3, 100 oC 1 h, 64% yield; (ii) Ar1-B(OH)2, Pd(PPh3)4, K2CO3, 1,4-Dioxane/H2O, 100 oC, overnight, 80%-72% yield; (iii) NaBH3CN, AcOH, 25oC, 5 min; (iv) Ar2-CH2Cl,K2CO3, MeCN, r.t., 4 h, 52%-42% yield; (v) ammonia 7 M in MeOH, 25 oC, 4 h, 80%-70% yield. (B) Chemical structures of mGlu2 NAMs 14a-14g.