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Table 1 Synthetic condition for preparation of [1111C] N -methyl-SSR504734

From: Synthesis and evaluation of 2-chloro N-[(S)-{(S)-1-[11 C]methylpiperidin-2-yl} (phenyl)methyl]3-trifluoromethyl-benzamide ([11 C]N-methyl-SSR504734) as a PET radioligand for glycine transporter 1

Entry

[11 C] methylating agent

Base

Solvent

Temperature

Time (min)

Yield (%)

1

[11 C]CH3I

NaH

DMF

r.t.

5

0

2

[11 C]CH3I

NaOH

DMF

r.t.

5

0

3

[11 C]CH3I

NaOH

DMF

80 °C

5

0

4

[11 C]CH3OTf

NaOH

Acetone

r.t.

1

25

5

[11 C]CH3OTf

NaOH

CH3CN

r.t.

1

36 to approximately 42

  1. DMF, dimethylformamide; r.t., room temperature.