We reported the incorrect structure for 13; it should be 2,3-difluoro not 2,3-dichloro. Correspondingly, 7 is 2,3-difluoro not 2,3-dichloro. The conclusions do not change, replacing the benzoxazole with imidazo[1,2-α]pyridine was deleterious (compare 13 and 8m, K_iapp = 160 and 19 nM, respectively). Corrected Scheme 1 and Table 3 are shown below. The following corrections should be made in the text: ^aReagents and conditions: (a) ArCHO, DarcoKB, O₂ (1 atm), xylene 140 °C, 6–8 h, 70–80%; (b) 10% Pd/C, H₂ (1 atm), EtOAc:MeOH, 3 h, 85–94%; (c) PPh₃, DEAD, (+)-methyl d-lactate, THF, 0 °C to rt, 4 h, 85–90%; (d) LiOH, THF:MeOH, 4 h, 86–91%; (e) 5, EDC·HCl, DMF, 12 h, 62–79%; (f) Lawesson’s reagent, 1,4-dioxane, reflux, 2 h, 71%; (g) DIBAL-H, DCM, −78 °C, 1 h, 89%; (h) 5 (Ar = 4-OMePh), NaBH(OAc)₃, DCE, 1.5 h, 81%; (i) 4-OMePhC(O)CH₂Br, NaHCO₃, EtOH, reflux, 12 h, 88%; (j) SnCl₂, EtOH:EtOAc, reflux, 2 h; (k) 7 (R = 2,3-diF), EDC·HCl, DMF, rt, 12 h, 60%; (l) 2-amino-4-nitrophenol, DABCO, NMP, 100 °C, 24 h, 60%; (m) 10% Pd/C, H₂, MeOH:EtOAc, 2–3 h; (n) 7 (R = 2,3-diCl), EDC·HCl, DMF, rt, 12 h, 67%; (o) l-alanine, CuI, Cs₂CO₃, DMF, 90 °C, 24 h; (p) 5 (Ar = 4-CNPh), HATU, DMF, rt, 12 h, 45–54%. ^aReagents and conditions: (a) ArCHO, DarcoKB, O₂ (1 atm), xylene 140 °C, 6–8 h, 70–80%; (b) 10% Pd/C, H₂ (1 atm), EtOAc:MeOH, 3 h, 85–94%; (c) PPh₃, DEAD, (+)-methyl d-lactate, THF, 0 °C to rt, 4 h, 85–90%; (d) LiOH, THF:MeOH, 4 h, 86–91%; (e) 5, EDC·HCl, DMF, 12 h, 62–79%; (f) Lawesson’s reagent, 1,4-dioxane, reflux, 2 h, 71%; (g) DIBAL-H, DCM, −78 °C, 1 h, 89%; (h) 5 (Ar = 4-OMePh), NaBH(OAc)₃, DCE, 1.5 h, 81%; (i) 4-OMePhC(O)CH₂Br, NaHCO₃, EtOH, reflux, 12 h, 88%; (j) SnCl₂, EtOH:EtOAc, reflux, 2 h; (k) 7 (R = 2,3-diF), EDC·HCl, DMF, rt, 12 h, 60%; (l) 2-amino-4-nitrophenol, DABCO, NMP, 100 °C, 24 h, 60%; (m) 10% Pd/C, H₂, MeOH:EtOAc, 2–3 h; (n) 7 (R = 2,3-diCl), EDC·HCl, DMF, rt, 12 h, 67%; (o) l-alanine, CuI, Cs₂CO₃, DMF, 90 °C, 24 h; (p) 5 (Ar = 4-CNPh), HATU, DMF, rt, 12 h, 45–54%. Values are the average and range of at least two independent determinations. Single determination. Page 4741, bottom right column: “carboxylic acid 7 (R = 2,3-diCl)” should read “carboxylic acid 7 (R = 2,3-diF)”. Page 4750, bottom left column: “(S)-2-(2,3-Dichlorophenoxy)-N-(2-(4-methoxyphenyl)imidazo-[1,2-α]pyridin-6-yl)propanamide (13)” should read “(S)-2-(2,3-Difluorophenoxy)-N-(2-(4-methoxyphenyl)imidazo-[1,2-α]pyridin-6-yl)propanamide (13)”. Page 4750, top right column: “acid 7 (R = 2,3-diCl, 1 mmol)” should read “acid 7 (R = 2,3-diF, 1 mmol). In the molecular formula strings and the associated biochemical and biological data (CSV) file the SMILE for compound 13 should be FC1 = C(O[C@@H](C)C(NC2═CN3C(C═C2)═NC(C4═CC═C(OC)C═C4)═C3)═O)C═CC═C1F In the NMR data file, p S-25, the structure should be replaced with This article has not yet been cited by other publications. ^aReagents and conditions: (a) ArCHO, DarcoKB, O₂ (1 atm), xylene 140 °C, 6–8 h, 70–80%; (b) 10% Pd/C, H₂ (1 atm), EtOAc:MeOH, 3 h, 85–94%; (c) PPh₃, DEAD, (+)-methyl d-lactate, THF, 0 °C to rt, 4 h, 85–90%; (d) LiOH, THF:MeOH, 4 h, 86–91%; (e) 5, EDC·HCl, DMF, 12 h, 62–79%; (f) Lawesson’s reagent, 1,4-dioxane, reflux, 2 h, 71%; (g) DIBAL-H, DCM, −78 °C, 1 h, 89%; (h) 5 (Ar = 4-OMePh), NaBH(OAc)₃, DCE, 1.5 h, 81%; (i) 4-OMePhC(O)CH₂Br, NaHCO₃, EtOH, reflux, 12 h, 88%; (j) SnCl₂, EtOH:EtOAc, reflux, 2 h; (k) 7 (R = 2,3-diF), EDC·HCl, DMF, rt, 12 h, 60%; (l) 2-amino-4-nitrophenol, DABCO, NMP, 100 °C, 24 h, 60%; (m) 10% Pd/C, H₂, MeOH:EtOAc, 2–3 h; (n) 7 (R = 2,3-diCl), EDC·HCl, DMF, rt, 12 h, 67%; (o) l-alanine, CuI, Cs₂CO₃, DMF, 90 °C, 24 h; (p) 5 (Ar = 4-CNPh), HATU, DMF, rt, 12 h, 45–54%. ^aReagents and conditions: (a) ArCHO, DarcoKB, O₂ (1 atm), xylene 140 °C, 6–8 h, 70–80%; (b) 10% Pd/C, H₂ (1 atm), EtOAc:MeOH, 3 h, 85–94%; (c) PPh₃, DEAD, (+)-methyl d-lactate, THF, 0 °C to rt, 4 h, 85–90%; (d) LiOH, THF:MeOH, 4 h, 86–91%; (e) 5, EDC·HCl, DMF, 12 h, 62–79%; (f) Lawesson’s reagent, 1,4-dioxane, reflux, 2 h, 71%; (g) DIBAL-H, DCM, −78 °C, 1 h, 89%; (h) 5 (Ar = 4-OMePh), NaBH(OAc)₃, DCE, 1.5 h, 81%; (i) 4-OMePhC(O)CH₂Br, NaHCO₃, EtOH, reflux, 12 h, 88%; (j) SnCl₂, EtOH:EtOAc, reflux, 2 h; (k) 7 (R = 2,3-diF), EDC·HCl, DMF, rt, 12 h, 60%; (l) 2-amino-4-nitrophenol, DABCO, NMP, 100 °C, 24 h, 60%; (m) 10% Pd/C, H₂, MeOH:EtOAc, 2–3 h; (n) 7 (R = 2,3-diCl), EDC·HCl, DMF, rt, 12 h, 67%; (o) l-alanine, CuI, Cs₂CO₃, DMF, 90 °C, 24 h; (p) 5 (Ar = 4-CNPh), HATU, DMF, rt, 12 h, 45–54%.

中文翻译：

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扩大基于苯并恶唑的肌苷 5'-单磷酸脱氢酶 (IMPDH) 抑制剂结构-活性作为潜在的抗结核药物

我们报告了13的错误结构；它应该是 2,3-二氟而不是 2,3-二氯。相应地，7是 2,3-二氟而不是 2,3-二氯。结论没有改变，用咪唑并 [1,2-α] 吡啶代替苯并恶唑是有害的（比较13和8m，K _{iapp 分别}为 160 和 19 nM）。修正后的方案 1 和表 3 如下所示。应在正文中进行以下更正：^a试剂和条件：(a) ArCHO、DarcoKB、O ₂ (1 atm)、二甲苯 140 °C、6–8 h、70–80%；(b) 10% Pd/C, H ₂ (1 atm), EtOAc:MeOH, 3 h, 85–94%; (c) PPh ₃ , DEAD, (+)-甲基d-乳酸，四氢呋喃，0 °C 至室温，4 小时，85–90%；(d) LiOH、THF:MeOH，4 小时，86–91%；(e) 5 , EDC·HCl, DMF, 12 h, 62–79%; (f) Lawesson 试剂，1,4-二恶烷，回流，2 小时，71%；(g) DIBAL-H, DCM, -78 °C, 1 h, 89%; (h) 5 (Ar = 4-OMePh)，NaBH(OAc) ₃，DCE，1.5 小时，81%；(i) 4-OMePhC(O)CH ₂ Br, NaHCO ₃ , EtOH, 回流, 12 h, 88%; (j) SnCl ₂，EtOH:EtOAc，回流，2h；(k) 7 (R = 2,3-diF), EDC·HCl, DMF, rt, 12 h, 60%; (l) 2-amino-4-nitrophenol, DABCO, NMP, 100 °C, 24 h, 60%; (m) 10% Pd/C, H ₂ , MeOH:EtOAc, 2–3 h; (n) 7 (R = 2,3-diCl), EDC·HCl, DMF, rt, 12 h, 67%; (o) l -丙氨酸、CuI、Cs ₂CO ₃，DMF，90℃，24小时；(p) 5 (Ar = 4-CNPh), HATU, DMF, rt, 12 h, 45–54%。^a试剂和条件：(a) ArCHO、DarcoKB、O ₂ (1 atm)、二甲苯 140 °C，6–8 h，70–80%；(b) 10% Pd/C, H ₂ (1 atm), EtOAc:MeOH, 3 h, 85–94%; (c) PPh ₃ , DEAD, (+)-甲基d-乳酸, THF, 0 °C to rt, 4 h, 85–90%; (d) LiOH、THF:MeOH，4 小时，86–91%；(e) 5 , EDC·HCl, DMF, 12 h, 62–79%; (f) Lawesson 试剂，1,4-二恶烷，回流，2 小时，71%；(g) DIBAL-H, DCM, -78 °C, 1 h, 89%; (h) 5 (Ar = 4-OMePh)，NaBH(OAc) ₃，DCE，1.5 小时，81%；(i) 4-OMePhC(O)CH ₂ Br, NaHCO ₃, EtOH, 回流, 12 h, 88% ; (j) SnCl ₂，EtOH:EtOAc，回流，2h；(k) 7 (R = 2,3-diF), EDC·HCl, DMF, rt, 12 h, 60%; (l) 2-amino-4-nitrophenol, DABCO, NMP, 100 °C, 24 h, 60%; (m) 10% Pd/C, H ₂ , MeOH:EtOAc, 2–3 h; (n) 7 (R = 2,3-diCl), EDC·HCl, DMF, rt, 12 h, 67%; (o) l-丙氨酸、CuI、Cs ₂ CO ₃、DMF，90°C，24小时；(p) 5 (Ar = 4-CNPh), HATU, DMF, rt, 12 h, 45–54%。数值是至少两个独立测定的平均值和范围。单定。第 4741 页，右下栏：“羧酸7 (R = 2,3-diCl)”应为“羧酸7(R = 2,3-diF)”。第 4750 页，左下栏：“(S)-2-(2,3-二氯苯氧基) -N- (2-(4-甲氧基苯基)咪唑-[1,2-α]吡啶-6-基)丙酰胺( 13 )”应改为“(S)-2-(2,3-二氟苯氧基) -N- (2-(4-甲氧基苯基)咪唑-[1,2-α]吡啶-6-基)丙酰胺( 13 )”。第 4750 页，右上栏：“酸7（R = 2,3-diCl，1 mmol）”应为“酸7（R = 2,3-diF，1 mmol）”。在分子式字符串和相关的生化和生物学数据 (CSV) 文件中，化合物13的 SMILE应为 FC1 = C(O[C@@H](C)C(NC2=CN3C(C=C2)=NC( C4=CC=C(O​​C)C=C4)=C3)=O)C=CC=C1F 在 NMR 数据文件中，p S-25，结构应替换为这篇文章还没有被其他出版物引用。^a试剂和条件：(a) ArCHO、DarcoKB、O ₂ (1 atm)、二甲苯 140 °C，6–8 h，70–80%；(b) 10% Pd/C, H ₂ (1 atm), EtOAc:MeOH, 3 h, 85–94%; (c) PPh ₃ , DEAD, (+)-甲基d-乳酸, THF, 0 °C to rt, 4 h, 85–90%; (d) LiOH、THF:MeOH，4 小时，86–91%；(e) 5 , EDC·HCl, DMF, 12 h, 62–79%; (f) Lawesson 试剂，1,4-二恶烷，回流，2 小时，71%；(g) DIBAL-H, DCM, -78 °C, 1 h, 89%; (h) 5 (Ar = 4-OMePh)，NaBH(OAc) ₃，DCE，1.5 小时，81%；(i) 4-OMePhC(O)CH ₂ Br, NaHCO ₃ , EtOH, 回流, 12 h, 88%; (j) 氯化锡₂, EtOH:EtOAc, 回流, 2 h; (k) 7 (R = 2,3-diF), EDC·HCl, DMF, rt, 12 h, 60%; (l) 2-amino-4-nitrophenol, DABCO, NMP, 100 °C, 24 h, 60%; (m) 10% Pd/C, H ₂ , MeOH:EtOAc, 2–3 h; (n) 7 (R = 2,3-diCl), EDC·HCl, DMF, rt, 12 h, 67%; (o) l-丙氨酸、CuI、Cs ₂ CO ₃、DMF，90°C，24小时；(p) 5 (Ar = 4-CNPh), HATU, DMF, rt, 12 h, 45–54%。^a试剂和条件：(a) ArCHO、DarcoKB、O ₂ (1 atm)、二甲苯 140 °C，6–8 h，70–80%；(b) 10% Pd/C, H ₂ (1 atm), EtOAc:MeOH, 3 h, 85–94%; (c) PPh ₃ , DEAD, (+)-甲基d-乳酸，四氢呋喃，0 °C 至室温，4 小时，85–90%；(d) LiOH、THF:MeOH，4 小时，86–91%；(e) 5 , EDC·HCl, DMF, 12 h, 62–79%; (f) Lawesson 试剂，1,4-二恶烷，回流，2 小时，71%；(g) DIBAL-H, DCM, -78 °C, 1 h, 89%; (h) 5 (Ar = 4-OMePh)，NaBH(OAc) ₃，DCE，1.5 小时，81%；(i) 4-OMePhC(O)CH ₂ Br, NaHCO ₃ , EtOH, 回流, 12 h, 88%; (j) SnCl ₂，EtOH:EtOAc，回流，2h；(k) 7 (R = 2,3-diF), EDC·HCl, DMF, rt, 12 h, 60%; (l) 2-amino-4-nitrophenol, DABCO, NMP, 100 °C, 24 h, 60%; (m) 10% Pd/C, H ₂ , MeOH:EtOAc, 2–3 h; (n) 7 (R = 2,3-diCl), EDC·HCl, DMF, rt, 12 h, 67%; (o) l -丙氨酸、CuI、Cs ₂CO ₃，DMF，90℃，24小时；(p) 5 (Ar = 4-CNPh), HATU, DMF, rt, 12 h, 45–54%。