96929-05-4 (乙基2-(叔丁氧羰基(甲基)氨基)噻唑-4-甲酸酯,ethyl 2-({[(tert-butoxy)carbonyl]amino}methyl)-1,3-thiazole-4-carboxylate)

_99%

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol

参考文献：

Biological evaluation of new largazole analogues: Alteration of macrocyclic scaffold with Click chemistry

Li, Xianlin; Tu, Zhenchao; Li, Hua; Liu, Chunping; Li, Zheng; et al, ACS Medicinal Chemistry Letters, 2013, 4(1), 132-136

合成路线：1 步

_92%

反应条件：

1.1 Reagents: Potassium bicarbonate Solvents: 1,2-Dimethoxyethane ; 15 min, rt
1.2 overnight, rt
1.3 Reagents: Pyridine Solvents: 1,2-Dimethoxyethane ; 15 min, 0 °C; 0 °C; 15 min, 0 °C
1.4 Reagents: Trifluoroacetic anhydride ; 3 h, 0 °C
1.5 Reagents: Triethylamine ; 2 - 3 h, rt

参考文献：

Synthesis, structure-activity analysis, and biological evaluation of sanguinamide B analogues

Wahyudi, Hendra; Tantisantisom, Worawan; Liu, Xuechao; Ramsey, Deborah M.; Singh, Erinprit K.; et al, Journal of Organic Chemistry, 2012, 77(23), 10596-10616

合成路线：1 步

_92%

反应条件：

1.1 Solvents: Diethyl ether

参考文献：

Depsipeptide analogs of the antitumor drug distamycin containing thiazole amino acid residues

Bailly, Christian; Houssin, Raymond; Bernier, Jean Luc; Henichart, Jean Pierre, Tetrahedron, 1988, 44(18), 5833-43

合成路线：1 步

_91%

反应条件：

1.1 Reagents: 2,6-Lutidine , Potassium bicarbonate , Trifluoroacetic anhydride ; -15 °C; -20 °C

参考文献：

Total synthesis of largazole

Ren, Qi; Dai, Lu; Zhang, Hui; Tan, Wenfei; Xu, Zhengshuang; et al, Synlett, 2008, (15), 2379-2383

合成路线：1 步

_89%

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol ; overnight, rt

参考文献：

Synthesis of the molecular hybrid inspired by Largazole and Psammaplin A

Yu, Xiaoling; Zhang, Bingbing; Shan, Guangsheng; Wu, Yue; Yang, Feng-Ling; et al, Tetrahedron, 2018, 74(5), 549-555

合成路线：1 步

85363-04-8

868-59-7

_85%

反应条件：

1.1 Reagents: Triethylamine Solvents: Methanol ; 3 h, 60 °C

参考文献：

Synthesis and biological activity of largazole and derivatives

Seiser, Tobias; Kamena, Faustin; Cramer, Nicolai, Angewandte Chemie, 2008, 47(34), 6483-6485

合成路线：1 步

_74%

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol ; overnight, rt

参考文献：

Process development and scale-up total synthesis of largazole, a potent class I histone deacetylase inhibitor

Chen, Qi-Yin; Chaturvedi, Pravin R.; Luesch, Hendrik, Organic Process Research & Development, 2018, 22(2), 190-199

合成路线：1 步

_74%

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol ; 6 h, 23 °C

参考文献：

Convergent and Modular Synthesis of Candidate Precolibactins. Structural Revision of Precolibactin A

Healy, Alan R.; Vizcaino, Maria I.; Crawford, Jason M.; Herzon, Seth B., Journal of the American Chemical Society, 2016, 138(16), 5426-5432

合成路线：1 步

_74%

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol ; 6 h, rt

参考文献：

CP0569, A New Broad-Spectrum Injectable Carbapenem. Part 1: Synthesis and Structure-Activity Relationships

Aihara, Kazuhiro; Kano, Yuko; Shiokawa, Sohjiro; Sasaki, Toshiro; Setsu, Fumihito; et al, Bioorganic & Medicinal Chemistry, 2003, 11(16), 3475-3485

合成路线：1 步

4530-20-5

_71%

反应条件：

1.1 Reagents: Diisopropylethylamine , BOP reagent Solvents: Dichloromethane ; 20 min, rt
1.2 Reagents: Ammonium hydroxide ; 2 h, rt
1.3 Reagents: Lawesson's reagent Solvents: Tetrahydrofuran ; 4 h, rt
1.4 Reagents: Sodium bicarbonate Solvents: Ethyl acetate ; rt
1.5 Reagents: Potassium bicarbonate Solvents: 1,2-Dimethoxyethane ; 15 min, rt
1.6 rt; 12 h, rt
1.7 Reagents: Pyridine Solvents: 1,2-Dimethoxyethane ; 0 °C; 10 min, 0 °C
1.8 Reagents: Trifluoroacetic anhydride ; 0 °C; 3 h, 0 °C; 0 °C → rt
1.9 Reagents: Triethylamine ; rt; 1 h, rt

参考文献：

RITA Mimics: Synthesis and Mechanistic Evaluation of Asymmetric Linked Trithiazoles

Pietkiewicz, Adrian L.; Zhang, Yuqi; Rahimi, Marwa N.; Stramandinoli, Michael; Teusner, Matthew; et al, ACS Medicinal Chemistry Letters, 2017, 8(4), 401-406

合成路线：1 步

_70%

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol ; 5 h, rt

参考文献：

Concise total synthesis of largazole

Xiao, Qiong; Wang, Li-Ping; Jiao, Xiao-Zhen; Liu, Xiao-Yu; Wu, Qian; et al, Journal of Asian Natural Products Research, 2010, 12(11-12), 940-949

合成路线：1 步

_67%

反应条件：

1.1 Solvents: Ethanol , Pyridine ; 6 h, reflux

参考文献：

Studies on synthesis of amino acid derived thiazoles. Preparation of bis-thiazoles as key fragments of aerucyclamide analogs

Fagundez, Catherine; Serra, Gloria, Heterocyclic Letters, 2013, 3(4), 415-426

合成路线：1 步

_65%

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol ; 7 h, rt

参考文献：

Radical-Mediated Thiol-Ene Strategy: Photoactivation of Thiol-Containing Drugs in Cancer Cells

Sun, Shuang; Oliveira, Bruno L.; Jimenez-Oses, Gonzalo; Bernardes, Goncalo J. L., Angewandte Chemie, 2018, 57(48), 15832-15835

合成路线：1 步

_65%

反应条件：

1.1 Reagents: Pyridine Solvents: Ethanol ; 24 h, reflux

参考文献：

Synthesis of a Microcystis aeruginosa predicted metabolite with antimalarial activity

Pena, Stella; Scarone, Laura; Manta, Eduardo; Stewart, Lindsay; Yardley, Vanessa; et al, Bioorganic & Medicinal Chemistry Letters, 2012, 22(15), 4994-4997

合成路线：1 步

_61%

反应条件：

1.1 Reagents: Potassium bicarbonate Solvents: 1,2-Dimethoxyethane
1.2 Reagents: 2,6-Lutidine , Trifluoroacetic anhydride Solvents: 1,2-Dimethoxyethane

参考文献：

Total synthesis of (+)-nostocyclamide

Moody, Christopher J.; Bagley, Mark C., Journal of the Chemical Society, 1998, (1998), 601-607

合成路线：1 步

_61%

反应条件：

1.1 Reagents: Potassium bicarbonate Solvents: 1,2-Dimethoxyethane
1.2 Reagents: 2,6-Lutidine , Trifluoroacetic anhydride

参考文献：

Total synthesis of (+)-nostocyclamide

Moody, Christopher J.; Bagley, Mark C., Synlett, 1996, (12), 1171-1172

合成路线：1 步

4530-20-5

_60%

反应条件：

1.1 Reagents: Ammonia , 2,2,2-Trichloroethyl chloroformate
1.2 Reagents: Lawesson's reagent
1.3 -

参考文献：

Synthesis of cyclohexapeptides as antimalarial and anti-trypanosomal agents

Pena, S.; Fagundez, C.; Medeiros, A.; Comini, M.; Scarone, L.; et al, MedChemComm, 2014, 5(9), 1309-1316

合成路线：1 步

_55%

反应条件：

1.1 Reagents: Potassium bicarbonate Solvents: 1,2-Dimethoxyethane ; -15 °C
1.2 Reagents: 2,6-Lutidine , Trifluoroacetic anhydride ; -10 °C

参考文献：

Total Synthesis of Microcin B17 via a Fragment Condensation Approach

Thompson, Robert E.; Jolliffe, Katrina A.; Payne, Richard J., Organic Letters, 2011, 13(4), 680-683

合成路线：1 步

_48%

反应条件：

1.1 Reagents: Potassium bicarbonate Solvents: 1,2-Dimethoxyethane
1.2 Reagents: Pyridine , Trifluoroacetic anhydride Solvents: 1,2-Dimethoxyethane

参考文献：

Utilization of Alternate Substrates by the First Three Modules of the Epothilone Synthetase Assembly Line

Schneider, Tanya L.; Walsh, Christopher T.; O'Connor, Sarah E., Journal of the American Chemical Society, 2002, 124(38), 11272-11273

合成路线：1 步

_42%

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol ; 15 min, -20 °C
1.2 8 h, rt

参考文献：

Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein

Patel, Bhargav A.; Abel, Biebele; Barbuti, Anna Maria; Velagapudi, Uday Kiran; Chen, Zhe-Sheng; et al, Journal of Medicinal Chemistry, 2018, 61(3), 834-864

合成路线：1 步

反应条件：

1.1 Reagents: Calcium carbonate Solvents: Ethanol ; 15 min, 0 °C
1.2 0 °C; 3 h, rt

参考文献：

Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities

Yao, Yiwu; Tu, Zhengchao; Liao, Chenzhong; Wang, Zhen; Li, Shang; et al, Journal of Medicinal Chemistry, 2015, 58(19), 7672-7680

合成路线：1 步

参考文献：

Product class 17: thiazoles

Kikelj, D.; Urleb, U., Science of Synthesis, 2002, 11, 627-833

合成路线：1 步

反应条件：

1.1 Solvents: Diethyl ether

参考文献：

Analog of dolastatin 3. Synthesis, proton NMR studies, and spatial conformation

Bernier, Jean Luc; Houssin, Raymond; Henichart, Jean Pierre, Tetrahedron, 1986, 42(10), 2695-702

合成路线：1 步

反应条件：

1.1 Solvents: Diethyl ether

参考文献：

A convenient method for the preparation of 2-(1-aminoalkyl)thiazole-4-carboxylic acids, key intermediates in the total synthesis of naturally occurring antitumor cyclopeptides

Houssin, Raymond; Lohez, Michele; Bernier, Jean Luc; Henichart, Jean Pierre, Journal of Organic Chemistry, 1985, 50(15), 2787-8

合成路线：1 步