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14.发明公开7β-아미노-3-[3-(4-치환된 테트라졸린-5-티온-1-일)프로펜-1-일]-3-세펨-4-카르복실산 유도체 및 그 제조방법 失效7β-氨基-3- [3-（4-取代的 - 四氢-5-硫酮困-1-基）丙烯-1-基〕-3-头孢烯-4-羧酸衍生物及其制造的方法
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公开(公告)号：KR1019910003184B1
公开(公告)日：1991-05-22
申请号：KR1019890000760
申请日：1989-01-25
Applicant: 한국과학기술연구원
IPC: C07D207/08 , C07D207/06
Abstract: proline derivative of formula (I) is prepared by reacting ethyl- 2-oxo-4- phenylbutenoate of formula (II) with L- alanyl-L-proline of formula (III) in the presence of a reducing agent selected from NaBH3CN or a mixture of Pd/C and H2 gas. The cpd. (I) has an angiotensin-converting enzyme inhibiting activity, and is useful as a hypotensive agent.
Abstract translation: 式（I）的脯氨酸衍生物通过式（II）的2-氧代-4-苯基丁烯酸乙酯与式（III）的L-丙氨酰-L-脯氨酸在选自NaBH 3 CN或 Pd / C和H2气体的混合物。 cpd。 （I）具有血管紧张素转化酶抑制活性，可用作降血压药。
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Patent Agency Ranking
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公开(公告)号：KR1019950008319B1
公开(公告)日：1995-07-27
申请号：KR1019920012642
申请日：1992-07-15
Applicant: 한국과학기술연구원
IPC: C07D501/20
Abstract: This is new cephalosphorin compd. and its parmaceutically acceptable salt of formula(I). In formula, R1 is H, or trityl, tert-butoxycarbonyl, or formyl; R2 H, p-methoxybenzyl, diphenylmethyl or salting compd. such as Na or K; R3 and R4 are same or different, and H, acetyl, or p-methoxybenzyl; X,Y are H, F, Cl, Br, or I; and Q hydrogen, chloro, vinyl, acetoxymethyl, halomethyl, pyridiniummethyl, N- ethyl pyridiniumyl thiomethyl, N- carboxymethyl pyridiniumyl thiomethyl, carbamoyloxymethyl, and N-methyl-tetrazolyl thiomethyl gp. This compd. is prepared by acylation of the aminothiazol compd of (II) with cephalosphorin of (III). This cephem compd. has good antibacterial activity.
Abstract translation: 这是新头孢菌素 和其药学上可接受的式（I）盐。 在式中，R 1是H或三苯甲基，叔丁氧基羰基或甲酰基; R2H，对甲氧基苄基，二苯甲基或盐析化合物。 如Na或K; R3和R4相同或不同，H，乙酰基或对甲氧基苄基; X，Y是H，F，Cl，Br或I; 和Q氢，氯，乙烯基，乙酰氧基甲基，卤代甲基，吡啶鎓甲基，N-乙基吡啶鎓硫代甲基，N-羧甲基吡啶鎓硫代甲基，氨基甲酰氧基甲基和N-甲基 - 四唑基硫代甲基gp。 这个compd 通过（II）的氨基噻唑化合物与（III）的头孢菌素的酰化制备。 这个cephem compd 具有良好的抗菌活性。
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公开(公告)号：KR1019950008318B1
公开(公告)日：1995-07-27
申请号：KR1019920012641
申请日：1992-07-15
Applicant: 한국과학기술연구원
IPC: C07D501/20
CPC classification number: Y02A50/473 , Y02A50/481
Abstract: This is new cephalosphorin compd. and its parmaceutically acceptable salt of formula(I). In formula, R1 is H, or trityl, tert-butoxycarbonyl, or formyl; R2 hydrogen, p-methoxybenzyl, diphenylmethyl, or salting compd. such as Na or K; R3 and R4 are same or different, and H, p-methoxybenzyl or diphenylmethyl; and Q hydrogen, chloro, vinyl, acetoxymethyl, halomethyl, N- ethylpyridiniumylthiomethyl, N- carboxymethyl pyridiniumyl thiomethyl, and N- methyl- tetrazolyl thiomethyl gp. This cephem compd. manufacturing method comprises A) condensing the amine compd. of (VIII) with ketone of (VII) and producing the compd of (II); and B) acylating the aminothiazol compd of (II) with cephalosphorin of (III). This cephem compd. has good antibacterial activity.
Abstract translation: 这是新头孢菌素 和其药学上可接受的式（I）盐。 在式中，R 1是H或三苯甲基，叔丁氧基羰基或甲酰基; R2氢，对甲氧基苄基，二苯基甲基或盐析化合物。 如Na或K; R3和R4相同或不同，H，对甲氧基苄基或二苯基甲基; 和Q氢，氯，乙烯基，乙酰氧基甲基，卤代甲基，N-乙基吡啶鎓硫基甲基，N-羧甲基吡啶鎓硫代甲基和N-甲基 - 四唑基硫代甲基gp。 这个cephem compd 制造方法包括：A）冷凝胺化合物。 （VIII）与（Ⅶ）的酮反应并制备（Ⅱ）化合物; 和B）用（III）的头孢菌素酰化（II）的氨基噻唑化合物。 这个cephem compd 具有良好的抗菌活性。
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公开(公告)号：KR1019930007813B1
公开(公告)日：1993-08-20
申请号：KR1019910018792
申请日：1991-10-25
Applicant: 한국과학기술연구원
IPC: C07D501/24
Abstract: Pyridonium alkenyl cephalosporin derivs. of formula (I) and their pharmaceutical salts are new. 3-Cephem compds. were obtained by witting reaction from a phosphonium cpd. of formula (II) with an aldehyde cpd. of formula (III) and then were deacylated to produce 7-amino-3-cephem derivs. The formula (I) derivs. are prepd. by acylation of 7-amino-3-cephem derivs. with 2- aminothiazolyl- 2-hydroxyimino-acetic acid compds. In (I), R1=H or a protecting gp. as in cephalosporin and penicillin cpds.; R2=H, C1-4 alkyl or substd. alkyl; R3=H or a deriv. of a carboxy gp., an atom for prepn. of a salt or carboxy protecting gp.
Abstract translation: 吡啶鎓烯基头孢菌素衍生物。 的式（I）化合物及其药用盐是新的。 3-Cephem compds 通过从cpd鏻反应得到。 式（II）与醛cpd反应。 的式（III），然后脱酰基以产生7-氨基-3-头孢烯衍生物。 公式（I）导出。 是prepd 通过7-氨基-3-头孢烯衍生物的酰化。 与2-氨基噻唑-2-基亚氨基 - 乙酸组成。 在（I）中，R1 = H或保护gp。 如头孢菌素和青霉素cpds。 R2 = H，C1-4烷基或取代基。 烷基; R3 = H或衍生物。 的羧基，一个原子的制备。 的盐或羧基保护gp。
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公开(公告)号：KR1019930007812B1
公开(公告)日：1993-08-20
申请号：KR1019910018791
申请日：1991-10-25
Applicant: 한국과학기술연구원
IPC: C07D501/24
Abstract: Alkenyl cephalosporin derivs. of formula (I) and their pharmaceutical salts are new. 3-cephem compds. were obtained by witting reaction from a phosphonium cpd. of formula (II) with an aldehyde cpd. of formula (III) and then were deacylated to produce 7- amino-3-cephem derivs. The formula (I) derivs. are prepd. by acylation of 7-amino-3-cephem derivs with 2- aminothiazolyl-2-hydroxyimino- acetic acid compds. In (I), R1=H or a protecting gp. as in cephalosporin and penicillin cpds.; R2=H, C1-4 alkyl or substd. alkyl; R3=H or a deriv. of a carboxy gp., an atom for prepn. of a salt or carboxy protecting gp.
Abstract translation: 烯基头孢菌素衍生物。 的式（I）化合物及其药用盐是新的。 3-头孢烯 通过从cpd鏻反应得到。 式（II）与醛cpd反应。 的式（III），然后脱酰基以产生7-氨基-3-头孢烯衍生物。 公式（I）导出。 是prepd 通过7-氨基-3-头孢烯衍生物与2-氨基噻唑-2-羟基亚氨基 - 乙酸化合物的酰化反应。 在（I）中，R1 = H或保护gp。 如头孢菌素和青霉素cpds。 R2 = H，C1-4烷基或取代基。 烷基; R3 = H或衍生物。 的羧基，一个原子的制备。 的盐或羧基保护gp。
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