公开(公告)号：KR100468314B1

公开(公告)日：2005-03-14

申请号：KR1020030069903

申请日：2003-10-08

Applicant: 화일약품주식회사

Inventor： 박태호 ,  양민승 ,  왕한철 ,  우혜경 ,  김종호 ,  윤진영

IPC: C07D207/14

Abstract: 본 발명에 의하여 식도의 괄약근압력을 증가시키고 식도연동운동을 촉진하며, 위장의 음식분쇄, 배출 등 소화작용을 촉진하며, 음식물의 소화관 이동시간을 빠르게 하는 약제인 구조식 (I)의 레보설피리드의 합성의 중간화합물인 다음 일반구조식 (Ⅳ) 및 그 제조방법을 제공한다.

公开(公告)号：KR100450485B1

公开(公告)日：2004-10-01

申请号：KR1020030069901

申请日：2003-10-08

Applicant: 화일약품주식회사

Inventor： 박태호 ,  양민승 ,  왕한철 ,  우혜경 ,  김종호 ,  윤진영

IPC: C07D207/14

Abstract: PURPOSE: An intermediate for preparing levosulpiride and a preparation method thereof are provided, thereby preparing levosulpiride in higher yield and purity. CONSTITUTION: An intermediate represented by the formula (V) for preparing levosulpiride of the formula (I) is provided, wherein R1 and R2 are independently hydrogen, C1-C4 lower alkyl or phenyl; R3 is phenyl derivative of the formula (VIII) or naphthyl derivative of the formula (IX); and X is hydrogen or halogen, provided that the formula (V) may be racemic body, (S) body and (R) body because it contains chiral carbon(*). A method for preparing an intermediate of the formula (V) for preparing levosulpiride comprises activating a compound of the formula (IV) in the presence of base using acid anhydride method, acid chloride method or azide method, and reacting the activated compound of the formula (IV) with 2-methoxy-5-sulfamoyl benzoic acid, wherein R1 and R2 are independently hydrogen, C1-C4 lower alkyl or phenyl; R3 is phenyl derivative of the formula (VIII) or naphthyl derivative of formula (IX); and X is hydrogen or halogen.

Abstract translation: 目的：提供一种制备左磺舒钠的中间体及其制备方法，由此以较高的收率和纯度制备左磺舒钠。 构成：提供了用于制备式（I）左磺舒醇酯的由式（V）表示的中间体，其中R 1和R 2独立地为氢，C 1 -C 4低碳烷基或苯基; R3是式（VIII）的苯基衍生物或式（IX）的萘基衍生物; X是氢或卤素，条件是式（V）可以是外消旋体，（S）体和（R）体，因为它含有手性碳（*）。 用于制备用于制备左磺柳碱的式（V）中间体的方法包括使用酸酐法，酰氯法或叠氮化物法在碱的存在下活化式（IV）的化合物，并且使活化的式 （IV）与2-甲氧基-5-氨磺酰基苯甲酸反应，其中R1和R2独立地为氢，C1-C4低级烷基或苯基; R3是式（VIII）的苯基衍生物或式（IX）的萘基衍生物; 并且X是氢或卤素。

公开(公告)号：KR1020030082526A

公开(公告)日：2003-10-22

申请号：KR1020030069903

申请日：2003-10-08

Applicant: 화일약품주식회사

Inventor： 박태호 ,  양민승 ,  왕한철 ,  우혜경 ,  김종호 ,  윤진영

IPC: C07D207/14

Abstract: PURPOSE: Provided are an intermediate for preparing levosulpiride and a preparation method thereof, thereby preparing levosulpiride in higher yield and purity. CONSTITUTION: An intermediate represented by the formula (IV) for preparing levosulpiride of the formula (I) is provided, wherein R1 and R2 are independently hydrogen, C1-C4 lower alkyl or phenyl; R3 is phenyl derivative of the formula (VIII) or naphthyl derivative of the formula (IX); and X is hydrogen or halogen, provided that the formula (IV) may be racemic body, (S) body and (R) body because it contains chiral carbon(*). A method for preparing an intermediate of the formula (IV) for preparing levosulpiride comprises reducing a compound of the formula (III) with a reducing agent, wherein R1 and R2 are independently hydrogen, C1-C4 lower alkyl or phenyl; R3 is phenyl derivative of the formula (VIII) or naphthyl derivative of the formula (IX); and X is hydrogen or halogen.

Abstract translation: 目的：提供制备左布舒地平的中间体及其制备方法，从而以更高的产率和纯度制备左布舒地尔。 构成：提供由式（IV）表示的用于制备式（I）的左布列脲的中间体，其中R 1和R 2独立地为氢，C 1 -C 4低级烷基或苯基; R3是式（VIII）的苯基衍生物或式（IX）的萘基衍生物; 并且X是氢或卤素，条件是式（IV）可以是外消旋体，（S）体和（R）体，因为它含有手性碳（*）。 制备式（IV）的中间体的方法，用于制备左旋肉豆蔻酸盐包括用还原剂还原式（III）化合物，其中R 1和R 2独立地是氢，C 1 -C 4低级烷基或苯基; R3是式（VIII）的苯基衍生物或式（IX）的萘基衍生物; X为氢或卤素。

公开(公告)号：KR100432587B1

公开(公告)日：2004-05-24

申请号：KR1020010031027

申请日：2001-06-02

Applicant: 화일약품주식회사

Inventor： 박태호 ,  양민승 ,  왕한철 ,  우혜경 ,  김종호 ,  윤진영

IPC: C07D207/14

Abstract: PURPOSE: Provided are a method for preparing Levosulpiride which increases the pressure of a sphincteral muscle, promotes the vermiculation of the gullet and facilitates digestion, in high yield and purity and intermediates used therein. CONSTITUTION: The method for preparing Levosulpiride of the formula(I) is characterized by treating a compound of the formula(V) with trifluoroacetate. In the formulae, R1 and R2 are independently hydrogen atom or 1-4 of lower alkyl or phenyl; R3 is a phenyl derivative of the formula(VIII) or naphthyl derivative of the formula(IX).

Abstract translation: 目的：提供一种制备左旋舒必利的方法，所述左旋舒必利增加肠内肌肉的压力，促进食道的蠕动并促进消化，其中以高收率和纯度以及其中使用的中间体。 构成：制备式（I）左磺舒醇酯的方法的特征在于用三氟乙酸盐处理式（V）化合物。 在通式中，R1和R2独立地为氢原子或1-4个低级烷基或苯基; R3是式（VIII）的苯基衍生物或式（IX）的萘基衍生物。

公开(公告)号：KR1020030082525A

公开(公告)日：2003-10-22

申请号：KR1020030069901

申请日：2003-10-08

Applicant: 화일약품주식회사

Inventor： 박태호 ,  양민승 ,  왕한철 ,  우혜경 ,  김종호 ,  윤진영

IPC: C07D207/14

Abstract: PURPOSE: An intermediate for preparing levosulpiride and a preparation method thereof are provided, thereby preparing levosulpiride in higher yield and purity. CONSTITUTION: An intermediate represented by the formula (V) for preparing levosulpiride of the formula (I) is provided, wherein R1 and R2 are independently hydrogen, C1-C4 lower alkyl or phenyl; R3 is phenyl derivative of the formula (VIII) or naphthyl derivative of the formula (IX); and X is hydrogen or halogen, provided that the formula (V) may be racemic body, (S) body and (R) body because it contains chiral carbon(*). A method for preparing an intermediate of the formula (V) for preparing levosulpiride comprises activating a compound of the formula (IV) in the presence of base using acid anhydride method, acid chloride method or azide method, and reacting the activated compound of the formula (IV) with 2-methoxy-5-sulfamoyl benzoic acid, wherein R1 and R2 are independently hydrogen, C1-C4 lower alkyl or phenyl; R3 is phenyl derivative of the formula (VIII) or naphthyl derivative of formula (IX); and X is hydrogen or halogen.

Abstract translation: 目的：提供一种制备左美沙比妥的中间体及其制备方法，从而以更高的产率和纯度制备左美沙非尼。 构成：提供由式（I）表示的式（Ⅴ）表示的中间体，其中R 1和R 2独立地为氢，C 1 -C 4低级烷基或苯基; R3是式（VIII）的苯基衍生物或式（IX）的萘基衍生物; 并且X是氢或卤素，条件是式（V）可以是外消旋体，（S）体和（R）体，因为它含有手性碳（*）。 制备式（Ⅴ）中间体的制备方法，包括使用酸酐法，酰氯法或叠氮化物法在碱的存在下活化式（Ⅳ）的化合物，并使式 （IV）与2-甲氧基-5-氨磺酰基苯甲酸，其中R 1和R 2独立地是氢，C 1 -C 4低级烷基或苯基; R3是式（VIII）的苯基衍生物或式（IX）的萘基衍生物; X为氢或卤素。

公开(公告)号：KR1020020092123A

公开(公告)日：2002-12-11

申请号：KR1020010031027

申请日：2001-06-02

Applicant: 화일약품주식회사

Inventor： 박태호 ,  양민승 ,  왕한철 ,  우혜경 ,  김종호 ,  윤진영

IPC: C07D207/14

Abstract: PURPOSE: Provided are a method for preparing Levosulpiride which increases the pressure of a sphincteral muscle, promotes the vermiculation of the gullet and facilitates digestion, in high yield and purity and intermediates used therein. CONSTITUTION: The method for preparing Levosulpiride of the formula(I) is characterized by treating a compound of the formula(V) with trifluoroacetate. In the formulae, R1 and R2 are independently hydrogen atom or 1-4 of lower alkyl or phenyl; R3 is a phenyl derivative of the formula(VIII) or naphthyl derivative of the formula(IX).

Abstract translation: 目的：提供一种制备左旋舒巴替罗的方法，其增加括约肌的压力，促进食道的呕吐并促进以高产率和纯度消化，以及其中使用的中间体。 构成：式（I）的左旋苏布里德的制备方法的特征在于用三氟乙酸盐处理式（V）的化合物。 在该式中，R 1和R 2独立地为氢原子或1-4个低级烷基或苯基; R3是式（VIII）的苯基衍生物或式（IX）的萘基衍生物。