تفاعل #61751

ord-e690c206e68c445d9f0bccfcc72a2c1e

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىpartitioned
  2. 2
    غسيلthe aqueous layer is washed with ether
  3. 3
    تجفيفThe combined organic layers are dried over MgSO4
  4. 4
    ترشيحfiltered
  5. 5
    تركيزconcentrated

الإجراء التجريبي

A solution of 3-(2-nitro-3-piperidin-1-yl-phenyl)-2-oxo-propionic acid ethyl ester (ii) in THF is treated with potassium ethoxide (“KOEt”) (1 eq), followed by bromoethyl pyruvate (1.05 eq), at 0° C. The reaction is allowed to warm to room temperature over 90 min. The reaction is diluted with water and ether, partitioned, and the aqueous layer is washed with ether. The combined organic layers are dried over MgSO4, filtered and concentrated. Chromatography gives 3-(2-nitro-3-piperidin-1-yl-phenyl)-2,5-dioxo-hexanedioic acid di ethyl ester (iii).

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07429603B2uspto-grants-2008_09