N-(piperidin-4-ylmethyl)acetamide

反応条件: temp:0.00; pressure:0.00; stir:

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

実験手順: 2-(1-sopropylpiperid-4-ylmethyl)-6-chloro-1,2-benzisothiazolin-3-one is obtained analogously to Example 33 by reacting 3-chloro-6-chlorocarbonylphenylsulfenyl chloride and 1-isopropyl-4-aminomethylpiperidine [boiling point 15 :95°-97° C.; obtained from 4-acetylaminomethylpiperidine and isopropyl chloride analogously to Singh et al., J. Med. Chem. 12, 949 (1969) and Werbel et al., supra]. After recrystallization in acetone, yellow crystals of melting point 134°-135° C. are obtained; yield: 37% of theory. 95°-97° C.

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

実験手順: 2-(1-sopropylpiperid-4-ylmethyl)-6-chloro-1,2-benzisothiazolin-3-one is obtained analogously to Example 33 by reacting 3-chloro-6-chlorocarbonylphenylsulfenyl chloride and 1-isopropyl-4-aminomethylpiperidine [boiling point 15 :95°-97° C.; obtained from 4-acetylaminomethylpiperidine and isopropyl chloride analogously to Singh et al., J. Med. Chem. 12, 949 (1969) and Werbel et al., supra]. After recrystallization in acetone, yellow crystals of melting point 134°-135° C. are obtained; yield: 37% of theory. 95°-97° C.

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

実験手順: 2-(1-sopropylpiperid-4-ylmethyl)-6-chloro-1,2-benzisothiazolin-3-one is obtained analogously to Example 33 by reacting 3-chloro-6-chlorocarbonylphenylsulfenyl chloride and 1-isopropyl-4-aminomethylpiperidine [boiling point 15 :95°-97° C.; obtained from 4-acetylaminomethylpiperidine and isopropyl chloride analogously to Singh et al., J. Med. Chem. 12, 949 (1969) and Werbel et al., supra]. After recrystallization in acetone, yellow crystals of melting point 134°-135° C. are obtained; yield: 37% of theory. 95°-97° C.

反応条件: temp:0.00; pressure:0.00; stir:

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

実験手順: Compound 279 is synthesized from Intermediate C and N-piperidin-4-ylmethyl-acetamide according to General Method H. (LC/MS method 16: ES+ m/z 382.4 [M+H]+, Rt=2.50 min)

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

実験手順: 2-(1-isopropylpiperid-4-ylmethyl)-6-chloro-1,2-benzisothiazolin-3-one is obtained analogously to Example 33 by reacting 3-chloro-6-chlorocarbonylphenylsulfenyl chloride and 1-isopropyl-4-aminomethylpiperidine [boiling point 15: 95°-97° C.; obtained from 4-acetylaminomethylpiperidine and isopropyl chloride analogously to Singh et al., J. Med. Chem. 12, 949 (1969) and Werbel et al., supra]. After recrystallization in acetone, yellow crystals of melting point 134°-135° C. are obtained; yield: 37% of theory. 95°-97° C.

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

実験手順: 2-(1-sopropylpiperid-4-ylmethyl)-6-chloro-1,2-benzisothiazolin-3-one is obtained analogously to Example 33 by reacting 3-chloro-6-chlorocarbonylphenylsulfenyl chloride and 1-isopropyl-4-aminomethylpiperidine [boiling point 15 :95°-97° C.; obtained from 4-acetylaminomethylpiperidine and isopropyl chloride analogously to Singh et al., J. Med. Chem. 12, 949 (1969) and Werbel et al., supra]. After recrystallization in acetone, yellow crystals of melting point 134°-135° C. are obtained; yield: 37% of theory. 95°-97° C.