NEW MATERIAL:A compound expressed by formula I (R1 is carboxy, cyano, hydroxymethyl, etc.; R2 is H, alkyl heteroaryl, benzyl, phenyl, etc.; R3 is H or alkyl; R4 is H or a protecting group of the carboxy group) and a salt thereof.
EXAMPLE: 4-Nitrobenzyl (5R, 6S)-6-[(1R)-hydroxyethyl]-2-[(2S, 4S)-2-carbamoyl-1-[(N-4-nitrobenzyloxycarbonyl)acetimidoyl]pyrrolidin-4-ylth-io]-2-carbapenem-3-carboxylate.
USE: An antimicrobial agent.
PREPARATION: A compound expressed by formula II (R4' has the same meaning as the protecting group in R4) is reacted with an anhydrous alkanesulfonic acid, etc., in the presence of a base to convert the group expressed by the formula =O into a group expressed by the formula -OR7 (R7 is alkanesulfonyl, etc.), and the resultant compound is then reacted with a compound expressed by formula III (R1' has the same meaning as R1 which may have protected amino group; R3' has the same meaning as R3 or is the protecting group of the amino group). The protecting groups are then removed to afford the aimed substance.
| WO/2008/079266 | SYNTHESIS OF PYRROLIDINE COMPOUNDS |
| JP2015535283 | Trans-clomiphene for use in cancer therapy |
| WO/2000/063157 | DISUBSTITUTED BENZENE DERIVATIVES |
HASHIMOTO TOSHIHIKO
TANAKA TERUO
IINO KIMIO
SHIBATA TOMOYUKI
MIYADERA TETSUO
SUGAWARA SHINICHI
| JPS5913757A | 1984-01-24 | |||
| JPS5916892A | 1984-01-28 | |||
| JPS59205379A | 1984-11-20 |