تفاعل #1833304

معادلة التفاعل

N-methylpyrrolidine

sodium

1,2,4-triazole

water

→

3-(1H-1,2,4-triazol-1-yl)-4,5-dihydroisoxazole

ظروف التفاعل

المعالجة

1. 1
   أخرىA microwave reaction
2. 2
   workup.ADDITIONvial is charged with racemic ompound
3. 3
   أخرىThe mixture was sealed
4. 4
   أخرىa brown solid crashes out which is isolated
5. 5
   ترشيحvacuum filtration
6. 6
   أخرىdried

الإجراء التجريبي

A microwave reaction vial is charged with racemic ompound I-10 (1.0 equiv) and the sodium salt of 1,2,4-triazole (2.0 equiv). The reagents are dissolved in N-methylpyrrolidine (0.18 M with respect to compound I-10). The mixture was sealed and heated in a microwave reactor at 100° C. for 30 min. Excess water is added and a brown solid crashes out which is isolated using vacuum filtration and dried to provide the desired 3-(1H-1,2,4-triazol-1-yl)-4,5-dihydroisoxazole I-34a and I-34b. These compounds can be separated using chiral HPLC methods known in the art. For example, see chiral HPLC Method disclosed herein. [M−H]−=306.1 m/z. Activity: C.

المصدر