95656-88-5 (N-CBZ-3-羟基吡咯啉,Benzyl 3-hydroxypyrrolidine-1-carboxylate)

_100%

反应条件：

1.1 Reagents: Triethylamine Solvents: Dichloromethane ; 45 min, -60 °C; -60 °C → rt; overnight, rt
1.2 Reagents: Hydrochloric acid Solvents: Water ; rt

参考文献：

Synthesis and biological studies of novel 2-aminoalkyl ethers as potential antiarrhythmic agents for the conversion of atrial fibrillation

Plouvier, Bertrand; Beatch, Gregory N.; Jung, Grace L.; Zolotoy, Alexander; Sheng, Tao; et al, Journal of Medicinal Chemistry, 2007, 50(12), 2818-2841

合成路线：1 步

_98%

反应条件：

1.1 Reagents: Sodium borohydride Solvents: Methanol ; 0 °C; 12 h, 0 °C → rt
1.2 Reagents: Sodium bicarbonate

参考文献：

Preparation of sulfonyl substituted (hetero)aromatic derivatives as RORγ inhibitors for treatment of autoimmune diseases

, China, , ,

合成路线：1 步

_95%

反应条件：

1.1 Reagents: Sodium hydroxide Solvents: Water ; rt → 0 °C
1.2 45 min, 0 °C; 4 h, rt
1.3 Reagents: Hydrochloric acid Solvents: Water ; pH 7 - 8

参考文献：

Novel spiroheterocyclic compounds [morpholine-4-carboxylic acid amides of heterocyclic cyclohexylalanine and neopentylglycine derivatives and their analogs], useful as reversible inhibitors of cysteine proteases such as cathepsin S

, World Intellectual Property Organization, , ,

合成路线：1 步

_94%

参考文献：

Preparation and in vitro and in vivo evaluation of quinolones with selective activity against Gram-positive organisms

Cooper, Curt S.; Klock, Pamela L.; Chu, Daniel T. W.; Hardy, Dwight J.; Swanson, Robert N.; et al, Journal of Medicinal Chemistry, 1992, 35(8), 1392-8

合成路线：1 步

86070-82-8

_90%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Tetrahydrofuran ; 16 h, rt

参考文献：

Preparation of azabicyclic derivatives of indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines for therapeutic use as α7-nACh receptor activators

, World Intellectual Property Organization, , ,

合成路线：1 步

86070-82-8

_87%

反应条件：

1.1 Reagents: Sodium carbonate Solvents: Tetrahydrofuran , Water ; 1 h, rt
1.2 Reagents: Hydrochloric acid Solvents: Water

参考文献：

Preparation of phenyl amino pyrimidine bicyclic compounds useful as protein kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

86070-82-8

_80%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Dichloromethane , Water ; rt; < 5 °C; 5 h, 25 °C

参考文献：

Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity

Wang, Jubo; Li, Tinghan; Zhao, Tengteng; Wu, Tizhi; Liu, Chuang; et al, European Journal of Medicinal Chemistry, 2019, 178, 782-801

合成路线：1 步

_75%

反应条件：

1.1 Reagents: Triethylamine Solvents: Dichloromethane ; 25 °C → 0 °C; 10 min, 0 °C
1.2 60 min, 0 °C

参考文献：

Pyrazolo[1,5-a]pyrimidine compounds as protein kinase inhibitors and their preparation, pharmaceutical compositions and their use in the treatment of protein kinase-mediated diseases

, United States, , ,

合成路线：1 步

_75%

反应条件：

1.1 Reagents: Triethylamine Solvents: Dichloromethane ; rt → 0 °C; 10 min, 0 °C
1.2 60 min, 0 °C

参考文献：

Preparation of novel pyrazolopyrimidines as cyclin dependent kinase inhibitors

, United States, , ,

合成路线：1 步

_57%

反应条件：

1.1 Reagents: Triethylamine Solvents: Dichloromethane ; 12 h, rt

参考文献：

Substituted pyridines as inhibitors of DNMT1 and their preparation

, World Intellectual Property Organization, , ,

合成路线：1 步

_52%

反应条件：

1.1 Reagents: Sodium borohydride Solvents: Methanol ; cooled; 2 h, rt
1.2 Solvents: Water ; rt

参考文献：

Preparation of substituted heterocyclyl amides as Rho-associated protein kinase inhibitor and their use for treating or preventing diseases mediated by the Rho-associated protein kinase

, United States, , ,

合成路线：1 步

_52%

反应条件：

1.1 Reagents: Sodium borohydride Solvents: Methanol ; rt; 2 h, rt

参考文献：

Preparation of Rho-associated protein kinase inhibitor

, World Intellectual Property Organization, , ,

合成路线：1 步

_52%

反应条件：

1.1 Reagents: Sodium borohydride Solvents: Methanol ; cooled; 2 h, rt
1.2 Solvents: Water ; rt

参考文献：

Rho-associated protein kinase inhibitor, pharmaceutical composition containing rho-associated protein kinase inhibitor, preparation method and use of the pharmaceutical composition

, World Intellectual Property Organization, , ,

合成路线：1 步

31970-04-4

_51%

反应条件：

1.1 Reagents: Borane Solvents: Tetrahydrofuran ; 0 °C; 16 h, rt; rt → 0 °C
1.2 Reagents: Sodium hydroxide , Hydrogen peroxide Solvents: Water ; 0 °C; 30 min, 0 °C; 2 h, rt
1.3 Reagents: Sodium bisulfite Solvents: Diethyl ether , Water ; 15 min

参考文献：

Preparation of 5-hydroxymethyloxazolidin-2-ones as antibacterials.

, United States, , ,

合成路线：1 步

31970-04-4

_51%