• Journal of Pharmaceutical Investigation
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• 제18권3호
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• pp.139-144
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• 1988

Piperacillin phthalidyl ester was synthesized by reacting piperacillin with triethylamine and bromophthalide in acetone and its chemical structure was determined by UV, IR, and PMR. The partition coefficient of the ester was increased and the ester was more lipophilic and less water soluble than piperacillin. The ester did not show the antimicrobial activity against Bacillus subtilis ATCC 6633 in vitro, but when hydrolyzed, the parent drug of ester, piperacillin, revealed antimicrobial activity in vivo. After a single oral dose of both piperacillin and the ester to rabbits, the serum piperacillin concentration was measured by bioassay. The ester exhibited improved pharmatokinetic characteristics: $T_{max}\;of\;2hr,\;C_{max}\;of\;4.26{\mu}g{\cdot}ml^{-1},K_{el}\;of\;0.057hr^{-1},\;and\;total\;AUC\;of\;85.42{\mu}g{\cdot}hr{\cdot}ml^{-1}$. Piperacillin on the other hand, did not exhibit any gastro-intestinal absorption.

• 한국응용과학기술학회지
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• 제24권3호
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• pp.211-218
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• 2007

Based on the Benzoflex (Vesicol Chemical Co.) as PVC plasticizer substituents for Di-n-octyl phthalate (DOP), a series of new aromatic carboxylic acid ester compounds were designed as plasticizers, synthesized, and screened for the endocrine disrupting activity. 2-Hydroxybenzoic acid (1) and 2-methoxybenzoic acid (2) as the commercially available starting materials were reacted with diethylene glycol (3) in the presence of p-toluenesulfonic acid using Dean-Stark column to give diethylene glycol di-(2-hydroxy)benzoate (4, KH01) and diethylene glycol di-(2-methoxy)benzoate (5, KH02), respectively. And diethylene glycol di-(3-pyridinyl) ester (7, KH03) and dipropylene glycol di-(3-pyridinyl) ester (9, KH04) were obtained in high yields by treatment of nicotinoyl chloride (6) with diethylene glycol (3) and dipropylene glycol (8) in the presence of triethylamine as a base. To determine the estrogenic disrupting effect of new synthetic phthalate analogues, E-screen assay method was used. Of these compounds, 4 (KH01) was found to be compound without endocrine disrupting effect.

• KSBB Journal
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• 제29권3호
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• pp.205-209
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• 2014

Chromatographic enantiomer resolution of chiral amines was performed on several covalently immobilized and coated chiral stationary phases (CSPs) based on polysaccharide derivatives under the mobile phase conditions containing base or acid or acid/base additive. The chromatographic parameters including separation factors and capacity factors were greatly influenced by the nature of the mobile phase containing base or acid or salt additive as well as the used CSPs. When 0.05% triethylamine/0.05% trifluoroacetic acid as an additive in the mobile phase was used on all CSPs in this study, the greatest enantiomer resolution was observed except for Chiralpak AD. Also, it was shown that the change of base additive into acid or salt in the mobile phase may directly affect chiral recognition mechanisms between the chiral selectors and analytes occurring during enantiomer separation, resulting in the change of elution orders.

• 한국수소및신에너지학회논문집
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• 제16권2호
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• pp.111-121
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• 2005

이 연구는 광화학적 물분해 수소제소 기술의 일환으로 수행 중인 광촉매와 바이오촉매를 복합한 시스템 활용 기술에서 광촉매가 갖는 물리적 특성의 영향을 파악하고자 진행되었다. 다양한 물리적 특성을 갖는 광촉매 얻기 위하여 상용광촉매, 수열화법(HT-TiON), 리고 저온합성법(LT-TiON) 등을 이용하여 샘플을 준비하였다. 가시광 감응을 위하여 암모니아나 triethylamine 처리를 하여 질소를 도핑도 시도하였다. 시도된 복합시스템은 인위적인 전자주개 없이 수소를 발생시키는 결과를 보여주었으나, 광촉매로부터 엔자임으로의 전자전달 부분이 율속단계로 확인되었다. 사용된 광촉매 샘플에 따라 수소발생량에 차이가 나타난 결과로 광촉매의 미세구조 (결정상, 결정도, 기공 크기 및 비표면적 등)이 중요한 역할을 하는 것으로 판단되었다. 얻어진 결과들을 활용하여 재료들이 고정화된 새로운 시스템 구성을 제안하였다.

• 대한화학회지
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• 제30권2호
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• pp.237-242
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• 1986

4-bromoiodobenzene 또는 4-diiodobenzene과 2 당량의 아크릴산 유도체들간의 트리에틸아민 존재하의 팔라듐 촉매를 이용한 비닐화 반응에 의해 (E,E)-p-Phenylene diacrylic acid유도체들을 비교적 좋은 수득율로 쉽게 얻을 수 있었다. 이들 반응에서 4-diiodobenzene이 4-bromoiodobenzene보다 더 좋은 반응성을 나타냈으며 이들 반응들은 입체특이성있게 진행되었다. 또한, 사용된 촉매에 다른 4-bromoiodobenzene의 선택적인 비닐화 반응을 이용하여 (E,E)-p-Phenylene diacrylic acid유도체들과 이외에 몇가지 1,4-diolefinic aromatic compounds를 편리하게 합성할 수 있었다.

• Bulletin of the Korean Chemical Society
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• 제35권8호
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• pp.2381-2384
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• 2014

A solid-phase synthetic approach is reported for the synthesis of an ascorbic acid (ASA)-dipeptide conjugate that exhibited enhanced antioxidant activity. The N-terminal amino group of dipeptide (Ala-Ala) on a resin support was first activated by 1,1'-carbonyldiimidazole (CDI), and then reacted with an ASA derivative. The addition of a base, triethylamine (TEA), promoted nucleophilic acylation of ASA derivative and yielded a desired product (ASA-Ala-Ala) with enhanced purity, when cleaved from the resin. Compared to the approach where a C3 hydroxyl group of ASA was first activated with CDI and then reacted with the amino group of dipeptide on the resin, this new approach allowed a significant reduction of a total reaction time from 120 h to 8 h at $25^{\circ}C$. As-prepared ASA-dipeptide conjugate (ASA-Ala-Ala) showed improved antioxidant activity compared to ASA.

• Archives of Pharmacal Research
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• 제17권4호
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• pp.281-283
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• 1994

5-sec-butylthiomethyl-5-alkyl (methyl or phenyl) hydantoins (3-x) were prepared by the reaction of sec-buylthiomethyl alkyl (methyl or phenyl) ketone (1-2), potassium cyanide and ammonium carbonate. 3-(2-Bromoethyl) hydantoins (5-6) were the reaction products of 5-sec-buythiomethyl-5-alkyl (methyl or phenyl) hydantoin and 1, 2-dibromothane in the presence of potassium hydroxide. Alkylation of 5 and 6 with an excess of alkyl (methyl or ethyl iodide in THF with sodium hydride as base gave three 1-alkyl (methyl or ethyl)-3-(2-bromoethyl) hydantoins (7-9). Treatment of the 2-bromothyl group with potassium thioacelate and triethylamine gave three 1-alkyl (methyl or ethyl)-3-92-acetylthioethyl) hydantoins (10-12). Hydrolysis of the 2-acetylthiuoethyl group with sodium hydroxide in methanol afforded the three 1-alkyl (methyl or ethyl)-3-(2-mercaptorthyl) hydantoins.

• 대한화학회지
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• 제27권6호
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• pp.441-448
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• 1983

여러가지 브롬화비닐 화합물들 ((Z)-1-bromopropene, 1-bromo-2-methylpropene, 2-bromo-3-methyl-2-butene, (E)-ethyl 2-methyl-3-bromo-2-propenoate, 1-bromo-cyclohexene)과 올레핀 화합물인 ethyl acrylate, methyl methacrylate, ethyl crotonate, allyl cyanide, ethyl 3-butenoate, ethyl 4-pentenoate와 methyl 10-undecenoate를 palladium acetate촉매와 triorthotolyphosphine 및 triehylamine존재 하의 수득율로 얻었으며 이들 생성물의 입체화학도 규명하였다. 위의 방법을 이용하므로써 ethyl 3-butenoate, ethyl 4-pentenoate와 methyl 10-undecenoate에 의한 4개, 5개 및 11개 탄소-탄소 결합의 확장도 가능하였다.

• 대한의용생체공학회:의공학회지
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• 제8권1호
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• pp.87-92
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• 1987

In order to evaluate the artificial skin for burn would covering materials, copoly(N. carbobenzoxy-L-Iysine-L-leucine)s were prepared by Ipolymerization of N - carbobenzoxy-L- I sine anhydride and L-leucine anhydride in homogeneous solvents using triethylamine as an initiator. The synthetic polypeptides and the oxter type polyurethane(PV)of medical grade were used as the sheet type membranes were prepared ; monolayer membrances were composed of only the polypeptides, bilayer membranes and blend membranes were controlled by composition of the polypeptides and PU. Test of the swelling degree, mechanical tensile strength, elongation, oxygen permeability, water-vapor loss and In vitro degradation treated by pretense TV of samples of artificial skin were measured by adequate methods so as to mechanical, physincal characterization and biodegradation. As a result, all the values of samples were found to be similar to desired value of skin which was nature. The Artificial skin based on polypeptides can be considered as ideal burn wound covering materials.

• 공업화학
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• 제8권6호
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• pp.1054-1057
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• 1997

염화아크릴로일과 여러 종류의 디아민을 트리에틸아민 존재하에서 Schotten-Baumann 반응에 의해 N,N'-비스아크릴아미드 유도체 4종을 합성하였고, IR, $^1H-NMR$, 원소분석을 통해 구조를 확인하였다. 합성한 N,N'-헥사메틸렌비스아크릴아미드(HMBA)와 N,N'-도데카메 틸렌비스아크릴아미드 (DMBA)의 수율은 56.0%와 70.4%로 디아민의 메틸렌기의 수가 증가할수록 높아졌다. 또한 N,N'-1,4-페닐렌비스아크릴아미드(PhBA)와 N,N'-비스아크릴아미드 유도체는 여러 종류의 가교고분자 제조에 이용될 수 있다.