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3-Haloindolenine의 반응성에 관한 연구(I)
천문우,김문환 대한약학회 1981 약학회지 Vol.25 No.3
Reaction of 3-chloroindolenine with acetic acid gives oxindole and acetoxyindole. Similar treatment of 3-bromoindolenine affords 6-bromoindole. Reaction of 3-chloro-and 3-bromoindolenine with methanolic sodium hydroxide gives 3-methoxyindolenine, 2-methoxyindolenine and oxindole. Thermal reaction of 3-bromoindolenine in 1, 1', 2, 2'-tetrachloroethane gives 6-bromoindole but no reaction is occurred in 3-chloroindolenine. Photolysis of 3-chloroindolenine gives indole, 4-, 5- and 7-chloroindole.
DMSO-Oxalyl Chloride에 의한 당의 산화
천문우 대한약학회 1983 약학회지 Vol.27 No.2
DMSO-oxalyl chloride at low temperature in methylene chloride reacted with isolated secondary hydroxyl groups in some monosaccharides to give alkoxysulfonium salts, convertible to carbonyls in high yields upon addition of triethylamine. And 1, 2:5, 6-di-O-isopropylidene-.alpha.- D-allofuranose which is the key intermediate in the synthesis of 3-O-acetyl-5-O-benzoyl- 2-deoxy-2- fluoro-D-arabinofuranosyl bromide, was also obtained by oxidizing 1, 2:5, 6-di-O-isopropylidene-.alpha.- D-glucofuranose with the oxidizing reagent, followed by reduction with sodium borohydride.
천문우,김문환,Chun, Moon-Woo,Kim, Moon-Hwan 대한약학회 1988 약학회지 Vol.32 No.3
Methyl 6-0-benzoyl-3-0-benzyl-2, 5-di-deoxy-2-fluoro-allofuranose (11) and 1, 2-0-di-acetyl-6-0-benzoyl-3, 5-di-deoxy-3-fluoro-glucofuranoes (22), sugar moieties of potential antiviral and/or anticancer chemotherapeutic nucleoside, were synthesized from D-glucose.
2-Deoxy-2-fluoro-D-arabinofuranose류의 합성 연구
천문우,김문환,김득준,정원근 대한약학회 1984 약학회지 Vol.28 No.3
A ten-step synthesis of 1, 3-di-O-acetyl-5-O-benzoyl-2-deoxy-2-fluoro-D-arabino-furanose, a versatile intermediate in the synthesis of chemotherapeutically important nucleosides, was achieved from D-glucose. This procedure affords good overall yields of products and is suitable for large scale preparations.
천문우,Cheon, Mun-U 한국과학기술단체총연합회 1999 과학과 기술 Vol.32 No.11
우리나라 기업이나 정부가 신약개발에 관심을 가진 것은 불과 10여년밖에 안되지만 국내 최초로 신약 1호가 SK제약과 SK케미칼에 의해 탄생되었다. 우리나라 신약개발 현황을 보면 임상단계가 1백40여건, 개량신약개발이 1백30여건, 임상1상 이상이 20여건 이지만 연구개발 환경에서 많은 문제점을 안고 있다. 신약개발을 가속화하기 위해선 기초연구에 보다 많은 투자가 필요하며 산ㆍ학ㆍ연의 협동연구체제 구축이 시급하다.
Isonicotinic acid hydrazide 誘導體의 合成 및 抗菌作用에 關한 硏究
千文宇 대구효성카톨릭대학 1971 연구논문집 Vol.8 No.1
Isonicotinic acid hydrazde(INAH) is wellknown chemotherapeutics as antubercular agent. And its good antitubercular action was reported by many workers. But that INAH produce the side action such as neuritis by formation Schiff's base with pyridoxine was reported. So in order to diminish this side action, several derivatives of INAH such as Sodium isonicotinic acid hydrazide methanesulfonate(IHMS), D-Glucuronolactone isonicotinyl hydrazone were synthesized and used in therapy of tuberculosis. Author's interst led to the synthesis of three new acyl derivatives of INAH such as N-(3.5-dinitorbenzoyl)-isonicitinic acid hydrazide, N-phenoxyacetyl-isonicotinic acid hydrazide and N-cinnamoyl-isonicotinic acid hydrazide. They were obtained by the action of 3,5-dinitrobenzoyl chloride, phenoxyacetyl chloride and cinnamoyl chloride with isonicotinic acid hydrazide in pyridine solution. And their in vitro antitubercular and antibacterial action test were carried out.
千文宇 대구효성가톨릭대학교 1973 연구논문집 Vol.12 No.1
Paper I of these studies has previously been reported in this journal. Author wishes to report now the influence of -CH=CH- group on the antibacterial activities. The relationship between the antibacterial activities and the chemical structure of 5-nitrofuran derivatives was reported in many studies. The antibacterial activity of 5-nitro furan derivatives depends mostly on the nitro radical of 5-position of furan ring, but the introduction of -CH=CH-group or-CH=N-group between the nitrofuryl group and the end group of side chain might result to enhance the antibacterial activity to some extent. Author's intrest led to the synthesis of five N4-furylacryl derivatives with -CH=CH-group in their structure and five N4-furoyl derivatives without the above group considering of the possibility of application this-CH=CH-group to the sulfonamides. The antibacterial activity tests will be carried out to compare the five N4-2-furylacry1 derivatives with the five N4-2-furoyl derivatives. Five N4-2-furylacryl derivatives such as N4-2-furylacryl-N1-2-pyrimidinyl sulfanilamide, N4-2-furylacryl-N1-(4-methyl-2-pyrimidinyl) sulfanilamide, n4-2-furylacryl-N1-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N4-2-furylacryl-N1-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide, N4-2-furylacryl-N1-2-thyazolylsulfanilamide and five N4-2-furoyl derivatives such as N4-2-furoyl-N1-2-pyrimidinyl sulfanilamide, N4-2-furoyl-N1-(4-methyl-2-pyrimidinyl) sulfanilamide, N4-2-furoyl-N1-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N4-2-furoyl-N1-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide and N4-2-furoyl-N1-thiazolyl sulfanilamide were synthesized. They were obtained by the action of N1-2-pyrimidinyl sulfanilamide, N1-(4-methyl-2-pyrimidinyl) sulfanilamide, N1-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N1-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide and N1-2-thiazolyl sulfanilamide with 2-furylacryl chloride and 2-furoyl chloride in 4% NaOH solution.