公开(公告)号：KR1020000011490A

公开(公告)日：2000-02-25

申请号：KR1019990026908

申请日：1999-07-05

Applicant: 한국화학연구원

Inventor： 정명희 ,  박준규 ,  조귀웅 ,  오정숙 ,  유복심 ,  공재양

IPC: C07D263/52

Abstract: PURPOSE: Title derivatives are prepared which has a good therapeutic activity of dys-mnesia and senile athymia as a muscarinic receptor agonist. CONSTITUTION: Title compounds (formula 1; X is oxygen atom or sulfur atom; R is hydrogen atom, halogen atom, nitro group, C1- C4 lower alkyl group or C1- C4 lower alkoxy group) and their pharmaceutical salts are prepared. Thus, 2.04 g of aminophenol is dissolved in ethanol anhydride at room temperature, followed by addition of 2.00 g 3-pyridine carboxaldehyde, 6.62 g of iodobenzene diacetate is added in the obtained solution, and concentrated under reduced pressure after 10 minutes to give 1.17 g of white title compounds.

Abstract translation: 目的：制备标题衍生物，其作为毒蕈碱受体激动剂具有良好的失眠症和老年不育症的治疗活性。 构成：制备标题化合物（式1; X为氧原子或硫原子; R为氢原子，卤素原子，硝基，C 1 -C 4低级烷基或C 1 -C 4低级烷氧基）及其药物盐。 因此，在室温下将2.04g氨基苯酚溶于乙醇酐中，然后加入2.00g 3-吡啶甲醛，在所得溶液中加入6.62g二乙酸碘苯，10分钟后减压浓缩，得到1.17g 的白色标题化合物。

公开(公告)号：KR100319490B1

公开(公告)日：2002-01-05

申请号：KR1019990026907

申请日：1999-07-05

Applicant: 한국화학연구원

Inventor： 정명희 ,  박준규 ,  조귀웅 ,  오정숙 ,  유복심 ,  정대영

IPC: C07D239/06 ,  A61K31/505

Abstract: 본발명은무스카린수용체작용물질(muscarinic receptor agonist)로서기억항진및 노인성치매치료제로유용한다음화학식 1로표시되는 1,2,3,4-테트라하이드로피리미딘유도체와이의약제학적으로허용가능한염, 그리고이의제조방법에관한것이다. 상기화학식 1에서 : R은 -H, -CH, -CHCH, -CH(CH)CH, -CHCH=CH, -CHC≡CH,,,또는을나타낸다.

公开(公告)号：KR100336971B1

公开(公告)日：2002-05-17

申请号：KR1019990026908

申请日：1999-07-05

Applicant: 한국화학연구원

Inventor： 정명희 ,  박준규 ,  조귀웅 ,  오정숙 ,  유복심 ,  공재양

IPC: C07D263/52

Abstract: 본발명은무스카린수용체작용물질(muscarinic receptor agonist)로서기억항진및 노인성치매치료제로유효한다음화학식 1로표시되는 1,2,5,6-테트라하이드로피리딜벤즈아졸유도체와이의약제학적으로허용가능한염, 그리고이들의제조방법에관한것이다. 상기화학식 1에서 : X는산소원자또는황원자를나타내고; R은수소원자, 할로겐원자, 니트로기, 탄소원자수 1 ∼ 4의저급알킬기또는탄소원자수 1 ∼ 4의저급알콕시기를나타낸다.

公开(公告)号：KR1020000011489A

公开(公告)日：2000-02-25

申请号：KR1019990026907

申请日：1999-07-05

Applicant: 한국화학연구원

Inventor： 정명희 ,  박준규 ,  조귀웅 ,  오정숙 ,  유복심 ,  정대영

IPC: C07D239/06 ,  A61K31/505

Abstract: PURPOSE: Title derivatives are prepared which has a good therapeutic activity of dys-mnesia and senile athymia. CONSTITUTION: Title compounds (formula 1; R is -H, -CH3, -CH2CH3, -CH2(CH2)3CH3, -CH2CH=CH2, etc.) and their pharmaceutical salt are prepared. Thus, 1.24 g of hydroxylamine hydrochloride is dissolved in water, and controlled to pH 7 by NaHCO3 saturated aqueous solution. The solution is refluxed for 2 hours in a mixed solution of 5-acetylpyrimidine and 50 ml of benzene using Dean-Stark column. Obtained solution is concentrated under reduced pressure to give 1.28 g of 1-pyrimidin-5-yl-(E)-ethanone oxime(yield 78 %).

Abstract translation: 目的：制备具有良好的失眠症和老年性无精症治疗活性的标题衍生物。 构成：制备标题化合物（式1; R为-H，-CH 3，-CH 2 CH 3，-CH 2（CH 2）3 CH 3，-CH 2 CH = CH 2等）及其药物盐。 因此，将1.24g盐酸羟胺溶于水中，并通过NaHCO 3饱和水溶液控制至pH7。 使用Dean-Stark柱，将溶液在5-乙酰基嘧啶和50ml苯的混合溶液中回流2小时。 得到的溶液在减压下浓缩，得到1.28g 1-嘧啶-5-基 - （E） - 乙酮肟（产率78％）。