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Application filed by 유영학, 주식회사 미 원filedCritical유영학
Priority to KR1019940007836ApriorityCriticalpatent/KR950029266A/en
Publication of KR950029266ApublicationCriticalpatent/KR950029266A/en
본 발명은 항생물질로 유용한 하기 구조식(Ⅰ)의 베타―락탐 유도체의 새로운 제조방법에 관한 것으로, 탈수, 건조시키지 않고 농축시킨 하기 구조식(Ⅴ)의 화합물과; C4위치의 카르복실산을 약염기성인 테트라메틸구아니딘으로 보호시킨 구조식(Ⅵ)의 7―아미노데스아세톡시세팔로스포란산을 pH 6.0∼8.5의 조건에서 아실화 시킴으로써 수율이 향상된 세프라딘 일수화물의 새로운 제조방법에 관한 것이다.The present invention relates to a novel process for preparing beta-lactam derivatives of the following structural formula (I) useful as antibiotics, comprising: compounds of the following structural formula (V) concentrated without dehydration and drying; Sepradinyl with improved yield by acylating 7-aminodesacetoxycephalosporranic acid of formula (VI) in which the carboxylic acid at the C 4 position is protected with weakly basic tetramethylguanidine at a pH of 6.0 to 8.5 It relates to a new process for producing hydrates.
Description
세프라딘 일수화물의 제조방법Process for preparing cepradine monohydrate
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.
Claims (1)
하기 구조식(Ⅱ)의 Dㅡ2―아미노―2―(1, 4―시클로헥사디에닐기)초산과 하기 구조식(Ⅲ)의 7―ADCA를 아실화 반응시켜 목적화합물(Ⅰ)을 제조함에 있어서, 탈수, 건조시키지 않고 농축시킨 하기 구조식(Ⅴ)의 화합물과; C4위치의 카르복실산을 보호기로 보호시킨 구조식(Ⅵ)의 7―ADCA을 직접 반응시켜 아실화시킨 다음 C4보호기를 제거함을 특징으로 하는 하기 구조식(Ⅰ)의 세프라딘 일수화물의 제조방법.In preparing the target compound (I) by acylating D2-2-amino-2- (1,4-cyclohexadienyl group) acetic acid of the following structural formula (II) with 7-ADCA of the following structural formula (III), A compound of formula (V) below concentrated without dehydration and drying; Preparation of the cepradine monohydrate of formula (I), characterized by directly reacting 7-ADCA of formula (VI) in which the carboxylic acid in the C 4 position is protected with acylation to remove a C 4 protecting group Way.※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.※ Note: This is to be disclosed by the original application.
KR1019940007836A1994-04-141994-04-14
Process for preparing cepradine monohydrate
KR950029266A
(en)
Process for producing alkali salt of /3s/-3-square bracket opened-figure bracket opened-/2-protected amino-4-thiazolyl/-acetyl-figure bracket closed -amino-square bracket closed-4-alkyl-2-oxo-1-azetidinyl-sulfonic acid