1,1-difluoro-4-isocyanatocyclohexane

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: This compound was prepared by using procedures analogous to those described for the synthesis of Example 5 starting from 1,1-difluoro-4-isocyanatocyclohexane and 4-(4-methylpiperazin-1-yl)-6-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrimidin-2-amine HCl salt. Analytic LCMS (M+H)+: m/z=486.2. This compound was prepared

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: A mixture of 4,4-difluorocyclohexanecarboxylic acid (0.20 g, 1.2 mmol) (Matrix Scientific, Cat. #018320), diphenylphosphonic azide (0.67 g, 2.4 mmol) (Aldrich, Cat. #178756) and triethylamine (0.51 mL, 3.6 mmol) in toluene (10 mL) was refluxed overnight. The volatiles were removed under reduced pressure to afford the product which was directly used for next step reaction without further purification. was refluxed overnight The volatiles were removed under reduced pressure to afford the product which was directly used for next step reaction without further purification

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: This compound was prepared by using procedures analogous to those described for the synthesis of Example 5 starting from 1,1-difluoro-4-isocyanatocyclohexane and 4-(4-methylpiperazin-1-yl)-6-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrimidin-2-amine HCl salt. Analytic LCMS (M+H)+: m/z=486.2. This compound was prepared

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: A mixture of 4,4-difluorocyclohexanecarboxylic acid (0.20 g, 1.2 mmol) (Matrix Scientific, Cat. #018320), diphenylphosphonic azide (0.67 g, 2.4 mmol) (Aldrich, Cat. #178756) and triethylamine (0.51 mL, 3.6 mmol) in toluene (10 mL) was refluxed overnight. The volatiles were removed under reduced pressure to afford the product which was directly used for next step reaction without further purification. was refluxed overnight The volatiles were removed under reduced pressure to afford the product which was directly used for next step reaction without further purification