3-[2-氯-4-(2-甲氧基-2-氧代乙基)苯基]-5-甲基-1,2-恶唑-4-羧酸合成路线 （共 7 条）
反应条件
trifluoroacetic acid
T=20°C; 4 h;
参考文献
Epple, Robert; Russo, Ross; Azimioara, Mihai; Cow, Christopher; Xie, Yongping; Wang, Xing; Wityak, John; Karanewsky, Don; Gerken, Andrea; Iskandar, Maya; Saez, Enrique; Martin Seidel; Tian, Shin-Shay
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 16 p. 4376 - 4380
反应条件
1.1: 55 percent / HCO2H / Raney-Ni / 10 h / 110 °C
2.1: 90 percent / NH2OH*HCl; Na2CO3 / H2O / 2 h / 20 °C
3.1: NCS; HCl / dimethylformamide / 0.5 h / 20 °C
4.1: KN(TMS)2; Et3N / diethyl ether / 1 h / 20 °C
4.2: Et3N / acetonitrile / 3 h / 0 °C
5.1: 100 percent / TFA / 4 h / 20 °C
View Scheme
参考文献
Epple, Robert; Russo, Ross; Azimioara, Mihai; Cow, Christopher; Xie, Yongping; Wang, Xing; Wityak, John; Karanewsky, Don; Gerken, Andrea; Iskandar, Maya; Saez, Enrique; Martin Seidel; Tian, Shin-Shay
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 16 p. 4376 - 4380
反应条件
1.1: 70 percent / Pd(Ph3P)4 / dimethylformamide / 30 h / 80 °C
2.1: 55 percent / HCO2H / Raney-Ni / 10 h / 110 °C
3.1: 90 percent / NH2OH*HCl; Na2CO3 / H2O / 2 h / 20 °C
4.1: NCS; HCl / dimethylformamide / 0.5 h / 20 °C
5.1: KN(TMS)2; Et3N / diethyl ether / 1 h / 20 °C
5.2: Et3N / acetonitrile / 3 h / 0 °C
6.1: 100 percent / TFA / 4 h / 20 °C
View Scheme
参考文献
Epple, Robert; Russo, Ross; Azimioara, Mihai; Cow, Christopher; Xie, Yongping; Wang, Xing; Wityak, John; Karanewsky, Don; Gerken, Andrea; Iskandar, Maya; Saez, Enrique; Martin Seidel; Tian, Shin-Shay
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 16 p. 4376 - 4380
反应条件
1.1: 100 percent / H2SO4 / 8 h / Heating
2.1: 95 percent / Et3N / CH2Cl2 / 1 h / 0 °C
3.1: 70 percent / Pd(Ph3P)4 / dimethylformamide / 30 h / 80 °C
4.1: 55 percent / HCO2H / Raney-Ni / 10 h / 110 °C
5.1: 90 percent / NH2OH*HCl; Na2CO3 / H2O / 2 h / 20 °C
6.1: NCS; HCl / dimethylformamide / 0.5 h / 20 °C
7.1: KN(TMS)2; Et3N / diethyl ether / 1 h / 20 °C
7.2: Et3N / acetonitrile / 3 h / 0 °C
8.1: 100 percent / TFA / 4 h / 20 °C
View Scheme
参考文献
Epple, Robert; Russo, Ross; Azimioara, Mihai; Cow, Christopher; Xie, Yongping; Wang, Xing; Wityak, John; Karanewsky, Don; Gerken, Andrea; Iskandar, Maya; Saez, Enrique; Martin Seidel; Tian, Shin-Shay
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 16 p. 4376 - 4380
反应条件
1.1: 95 percent / Et3N / CH2Cl2 / 1 h / 0 °C
2.1: 70 percent / Pd(Ph3P)4 / dimethylformamide / 30 h / 80 °C
3.1: 55 percent / HCO2H / Raney-Ni / 10 h / 110 °C
4.1: 90 percent / NH2OH*HCl; Na2CO3 / H2O / 2 h / 20 °C
5.1: NCS; HCl / dimethylformamide / 0.5 h / 20 °C
6.1: KN(TMS)2; Et3N / diethyl ether / 1 h / 20 °C
6.2: Et3N / acetonitrile / 3 h / 0 °C
7.1: 100 percent / TFA / 4 h / 20 °C
View Scheme
参考文献
Epple, Robert; Russo, Ross; Azimioara, Mihai; Cow, Christopher; Xie, Yongping; Wang, Xing; Wityak, John; Karanewsky, Don; Gerken, Andrea; Iskandar, Maya; Saez, Enrique; Martin Seidel; Tian, Shin-Shay
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 16 p. 4376 - 4380
反应条件
1.1: 90 percent / NH2OH*HCl; Na2CO3 / H2O / 2 h / 20 °C
2.1: NCS; HCl / dimethylformamide / 0.5 h / 20 °C
3.1: KN(TMS)2; Et3N / diethyl ether / 1 h / 20 °C
3.2: Et3N / acetonitrile / 3 h / 0 °C
4.1: 100 percent / TFA / 4 h / 20 °C
View Scheme
参考文献
Epple, Robert; Russo, Ross; Azimioara, Mihai; Cow, Christopher; Xie, Yongping; Wang, Xing; Wityak, John; Karanewsky, Don; Gerken, Andrea; Iskandar, Maya; Saez, Enrique; Martin Seidel; Tian, Shin-Shay
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 16 p. 4376 - 4380
反应条件
1.1: NCS; HCl / dimethylformamide / 0.5 h / 20 °C
2.1: KN(TMS)2; Et3N / diethyl ether / 1 h / 20 °C
2.2: Et3N / acetonitrile / 3 h / 0 °C
3.1: 100 percent / TFA / 4 h / 20 °C
View Scheme
参考文献
Epple, Robert; Russo, Ross; Azimioara, Mihai; Cow, Christopher; Xie, Yongping; Wang, Xing; Wityak, John; Karanewsky, Don; Gerken, Andrea; Iskandar, Maya; Saez, Enrique; Martin Seidel; Tian, Shin-Shay
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 16 p. 4376 - 4380
