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公开(公告)号：KR1020000049811A
公开(公告)日：2000-08-05
申请号：KR1020000023417
申请日：2000-05-02
IPC: C07B55/00
CPC classification number: C07B55/00
Abstract: PURPOSE: A stereo-selective method for preparing (R)-(-)-muscone with high optical purity and high yield is provided. CONSTITUTION: A method for preparing (R)-(-)-muscone comprises steps of: (i) reacting 4-(cis-2, 6-dimethylpiperidine)-(R)-dinaphtodioxaphosphepin of the following formula (I) and 4-(R, R-2, 5-diphenylpyrrolidine)-(R)-dinaphtodioxaphosphepin of the following formula (II) with Cu(OTf)2 to form a complex with copper; and (ii) 1, 4-addition reacting dimethylzinc with 2-cyclopentadecenone using the complex of step (i) as a chiral catalyst.
Abstract translation: 目的：提供用于制备具有高光学纯度和高产率的（R） - （ - ） - 肌肉的立体选择性方法。 构成：制备（R） - （ - ） - 肌肉酮的方法包括以下步骤：（i）使下式（I）的4-（顺式-2,6-二甲基哌啶） - （R） - 二盐基二磷杂螺环和4- （II）的（R，R-2,5-二苯基吡咯烷） - （R） - 二萘氧基磷杂苯基与Cu（OTf）2形成与铜的络合物; 和（ii）使用步骤（i）的络合物作为手性催化剂，使二甲基锌与2-环戊烯酮1,4-加成反应。
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公开(公告)号：KR100340760B1
公开(公告)日：2002-06-20
申请号：KR1020000023417
申请日：2000-05-02
IPC: C07B55/00
Abstract: 본 발명은 4-(시스-2,6-다이메틸피페리딘)-(R)-다이나프토다이옥사포스페핀(Ⅰ), 4-(R,R-2,5-다이페닐피롤리딘)-(R)-다이나프토다이옥사포스페핀(Ⅱ)을 구리(Ⅱ)트리플레이트와 반응시켜 구리와 복합체를 형성하고, 이를 키랄 촉매로 사용하여 다이메틸징크를 2-시클로펜타데세논과 1,4-첨가반응시켜 고 광학순도, 고 수율로 (R)-(-)-무스콘(
l -muscone)을 입체선택적으로 제조하는 방법을 제공하는 것이다.-
公开(公告)号：KR1020000028355A
公开(公告)日：2000-05-25
申请号：KR1019980046559
申请日：1998-10-31
Applicant: 우리켐테크(주)
IPC: C07C49/607
Abstract: PURPOSE: A process for producing cyclopentadec-2-enone as a useful intermediate for the synthesis of muscone as an aromatic component of natural musk is provided which can produce the title compound in high purity and yield without purification processes. CONSTITUTION: A process comprises the steps of (a) producing 2-phenyl selenyl cyclopentadecanone by reacting cyclopentadecanone with diphenylselenide and selenium dioxide in the presence of an acid and (b) producing cyclopentadec-2-enone by reacting 2-phenyl selenyl cyclopentadecanone with an oxidant in the presence of a base. The acid is a Lewis acid such as sulfuric acid or trifluoroboron.diethylether(BF3.OEt2), the oxidant is hydrogen peroxide, peroxybenzoate, methachloroperbenzoic acid or oxone and the base is pyridine or imidazole.
Abstract translation: 目的：提供一种生产环戊十烯-2-酮作为天然麝香的芳族成分的肌醇合成有用中间体的方法，可以无需纯化即可生产高纯度和无收率的标题化合物。 构成：一种方法包括以下步骤：（a）在酸存在下使环十五烷酮与二苯基硒和二氧化硒反应制备2-苯基烯丙基环十五烷，和（b）通过2-苯基烯丙基环十五烷与 氧化剂在碱的存在下。 酸是路易斯酸如硫酸或三氟硼烷二乙醚（BF 3 OEt 2），氧化剂是过氧化氢，过氧苯甲酸酯，甲基氯过苯甲酸或丁酮，碱是吡啶或咪唑。
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公开(公告)号：KR100275039B1
公开(公告)日：2000-12-15
申请号：KR1019980046559
申请日：1998-10-31
Applicant: 우리켐테크(주)
IPC: C07C49/607
Abstract: 본 발명은 천연사향의 방향성분인 무스콘의 합성에 유용한 중간체인 시클로펜타덱-2-에논의 제조방법에 관한 것으로, 본 발명의 방법은 (a) 촉매량의 산존재하에 시클로펜타데카논에 디페닐셀레나이드와 셀레늄디옥사이드를 반응시켜 2-페닐셀레닐시클로펜타데카논을 생성하는 단계와, (b) 2-페닐셀레닐시클로펜타데카논을 염기의 존재하에서 산화제와 반응시켜 목적화합물인 시클로펜타덱-2-에논을 생성하는 단계로 이루어진다.
본 발명의 방법에 의하면, 간단한 2단계 공정에 의해 분리,정제공정없이도 고순도의 시클로펜타덱-2-에논을 고수율로 제조할 수 있다.-
公开(公告)号：KR1020020017165A
公开(公告)日：2002-03-07
申请号：KR1020000050327
申请日：2000-08-29
Applicant: 한국과학기술원
IPC: C07F7/18
CPC classification number: C07F7/1804
Abstract: PURPOSE: Provided are a novel (S)-2-t-butyldiphenylsilyloxymethylindoline of the formula(1) and a process for preparing (2S,3S)-2,3-dialkyltartaric acid by pinacol coupling using it as a chiral ligand, thereby producing (2S,3S)-2,3-dialkyltartaric acid in high chemical and optical yields. CONSTITUTION: (S)-2-t-butyldiphenylsilyloxymethylindoline is represented by the formula(1), wherein R is methyl or phenyl, and prepared by the steps of: reducing (S)-indoline-2-carbonic acid into lithium aluminum hydride; reacting it with chloro t-butyldiphenylsilane compound in the presence of imidazole to obtain (S)-2-t-butyldiphenylsilyloxymethylindoline. (2S,3S)-2,3-dialkyltartaric acid is prepared by the steps of: reacting 2-keto carbonic acid with (S)-2-t-butyldiphenylsilyloxymethylindoline(I) in the presence of dicyclohexylcarbodiimide(DDC) to obtain 2-ketoamide(II); pinacol coupling the 2-ketoamide(II) in the presence of hexamethylphosphoamide(HMP) to obtain dialkyltartaric acid derivative; and hydrolyzing the derivative to manufacture (2S,3S)-2,3-dialkyltartaric acid(III).
Abstract translation: 目的：提供式（1）的新型（S）-2-叔丁基二苯基甲硅烷氧基甲基二氢吲哚和通过频哪醇偶联使其作为手性配体制备（2S，3S）-2,3-二烷基酒石酸的方法，从而产生 （2S，3S）-2,3-二烷基酒石酸，具有高的化学和光学收率。 构成：（S）-2-叔丁基二苯基甲硅烷氧基甲基二氢吲哚由式（1）表示，其中R是甲基或苯基，并通过以下步骤制备：将（S） - 二氢吲哚-2-碳酸还原成氢化铝锂; 在咪唑存在下与氯代叔丁基二苯基硅烷化合物反应，得到（S）-2-叔丁基二苯基甲硅烷氧基甲基二氢吲哚。 （2S，3S）-2,3-二烷基酒石酸通过以下步骤制备：在二环己基碳二亚胺（DDC）的存在下，使2-酮基碳酸与（S）-2-叔丁基二苯基甲硅烷氧基甲基二氢吲哚（I）反应，得到2- 酮酰胺（II）; 频烯醇在六甲基磷酰胺（HMP）的存在下偶联2-酮酰胺（II），得到二烷基酒石酸衍生物; 并水解该衍生物制备（2S，3S）-2,3-二烷基酒石酸（III）。
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Patent Agency Ranking
公开(公告)号：KR100204659B1
公开(公告)日：1999-06-15
申请号：KR1019960018134
申请日：1996-05-28
IPC: C07D489/02
CPC classification number: C07D489/12
Abstract: 본 발명은 테바인을 출발물질로 하여 합성된 일반식(Ⅰ)의 진통제 화합물에 관한 것이다.
상기식에서 R은 수소, 메틸, 에틸 또는 시클로프로필이다.-
公开(公告)号：KR1019920018034A
公开(公告)日：1992-10-21
申请号：KR1019910003947
申请日：1991-03-12
Applicant: 한국과학기술원
IPC: C07D251/56
Abstract: 내용 없음
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公开(公告)号：KR1019900007247B1
公开(公告)日：1990-10-06
申请号：KR1019880001077
申请日：1988-02-05
Applicant: 한국과학기술원
IPC: C07D489/02
Abstract: A process for preparing buprenorphine of formula (I) comprises (A) oxidation of a cyan compound in 30% H2O2 soln. and NaOH soln. to form a urea cpd. (II), (B) reaction of (II) with KOH in the presence of diethyleneglycol to form a amine cpd. (III), (C) reaction of (III) with halomethylcyclopropane in the presence of K2CO3 and organic solvent, (D) reaction of the resultant cpd. with base in organic solvent to form (I). (I) is useful as an analgesic being antagonistic to narcotic addict.
Abstract translation: 制备式（I）的丁丙诺非的方法包括（A）在30％H 2 O 2溶胶中氧化青色化合物。 和NaOH溶液。 形成尿素cpd。 （II），（B）在二甘醇存在下，（II）与KOH的反应形成胺cpd。 （III），（C）在（K 3 CO 3）和有机溶剂存在下，（III）与卤代甲基环丙烷的反应，（D）所得cpd的反应。 用碱在有机溶剂中形成（I）。 （I）可用作与麻醉药成瘾者拮抗的止痛剂。
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公开(公告)号：KR1020020017166A
公开(公告)日：2002-03-07
申请号：KR1020000050328
申请日：2000-08-29
Applicant: 한국과학기술원
IPC: C07F7/18
CPC classification number: C07F7/1804
Abstract: PURPOSE: Provided are a novel (2S,3aS,7aS)-2-(t-butyldiphenylsilyloxymethyl)octahydroindoline of the formula(1) and a process for preparing (2R,3R)-2,3-dialkyltartaric acid by pinacol coupling using it as a chiral ligand, thereby producing (2R,3R)-2,3-dialkyltartaric acid in high chemical and optical yields. CONSTITUTION: (2S,3aS,7aS)-2-(t-butyldiphenylsilyloxymethyl)octahydroindoline is represented by the formula(1), wherein R is methyl or phenyl, and prepared by the steps of: converting (S)-indoline-2-carbonic acid into (S)-indoline-2-carbonic acid ethyl ester using thionyl chloride and ethanol; reducing it by using platinum oxide to obtain (2S,3aS,7aS)-octahydroindole-2-carbonic acid ethyl ester; reducing it by using lithium aluminum hydride; reacting it with chloro t-butyldiphenylsilane acid in the presence of imidazole to obtain (2S,3aS,7aS)-2-(t-butyldiphenylsilyloxymethyl)octahydroindoline. (2R,3R)-2,3-dialkyltartaric acid is prepared by the steps of: reacting 2-keto carbonic acid with (2S,3aS,7aS)-2-(t-butyldiphenylsilyloxymethyl)octahydroindoline(I) in the presence of dicyclohexylcarbodiimide(DDC) to obtain 2-ketoamide(II); pinacol coupling the 2-ketoamide(II) in the presence of hexamethylphosphoamide(HMP) to obtain dialkyltartaric acid derivative; and hydrolyzing the derivative to manufacture (2R,3R)-2,3-dialkyltartaric acid(III).
Abstract translation: 目的：提供式（1）的新型（2S，3aS，7aS）-2-（叔丁基二苯基甲硅烷氧基甲基）八氢二氢吲哚和通过频闪偶联使用其制备（2R，3R）-2,3-二烷基酒石酸的方法 作为手性配体，从而以高的化学和光学收率产生（2R，3R）-2,3-二烷基酒石酸。 构成：（2S，3aS，7aS）-2-（叔丁基二苯基甲硅烷氧基甲基）八氢二氢吲哚由式（1）表示，其中R是甲基或苯基，并通过以下步骤制备：将（S） - 二氢吲哚-2- 使用亚硫酰氯和乙醇将碳酸转化成（S） - 二氢吲哚-2-碳酸乙酯; 通过使用氧化铂将其还原，得到（2S，3aS，7aS） - 八氢吲哚-2-碳酸乙酯; 使用氢化铝锂还原它; 在咪唑存在下与氯叔丁基二苯基硅烷反应，得到（2S，3aS，7aS）-2-（叔丁基二苯基甲硅烷氧基甲基）八氢二氢吲哚。 （2R，3R）-2,3-二烷基酒石酸通过以下步骤制备：使2-酮碳酸与（2S，3aS，7aS）-2-（叔丁基二苯基甲硅烷氧基甲基）八氢二氢吲哚（I）在二环己基碳二亚胺 （DDC）得到2-酮酰胺（II）; 频烯醇在六甲基磷酰胺（HMP）的存在下偶联2-酮酰胺（II），得到二烷基酒石酸衍生物; 并水解该衍生物制备（2R，3R）-2,3-二烷基酒石酸（III）。
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公开(公告)号：KR100302325B1
公开(公告)日：2001-11-22
申请号：KR1019980051031
申请日：1998-11-26
Applicant: 한국과학기술원
IPC: C07D405/04
Abstract: 본 발명은 항암제인 독시플루리딘의 새로운 합성방법에 관한 것으로서 보다 상세하게는 2',3'-아세틸-5-플루오로유리딘을 메탄설포닐 클로라이드로 메실화시켜 2',3'-아세틸-5'-메실-5-플루오로유리딘을 합성하고, 여기에 금속아연과 요오드화 나트륨으로 반응시켜 2',3'-아세틸-5'-디옥시-5-플루오로유리딘을 합성하고 이것을 탈보호화시켜서 독시플루리딘을 합성하는 것을 특징으로 하는 독시플루리딘 제조 방법에 관한 것이다.
또한 본 발명인 독시플루리딘을 합성하는데 있어서 저가이면서 독성이 적은 메탄설포닐 클로라이드, 금속아연, 요오드화 나트륨 외에 초음파를 사용함으로써 독시플루리딘의 수율을 높일 수 높다.
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