[특허]Amino alcohol derivative and method for preparing the same

[미국특허] Amino alcohol derivative and method for preparing the same 원문보기

IPC분류정보
국가/구분	United States(US) Patent 등록
국제특허분류(IPC7판)	C07D-207/12
출원번호	US-0255869 (1999-02-23)
우선권정보	JP-0345080 (1995-12-08)
발명자 / 주소	Masayuki Jinbo JP Hidekazu Oyamada JP Jinichi Inokuchi JP
출원인 / 주소	Seikagaku Kogyo Kabushiki Kaisha JP
대리인 / 주소	Sughrue, Mion, Zinn, Macpeak & Seas, PLLC
인용정보	피인용 횟수 : 30 인용 특허 : 2

초록 ▼

A process for preparing a 2-acylamino alcohol derivative which comprises (A) reacting an aminopropanol derivative represented by the following formula (1):Y-CH2-C*H (NHP1)-C*H(OH)-R1 (1) with an amine represented by R2H to synthesize an amino alcohol derivative represented by the following formula (2):R2-CH2-C*H(NHP1)-C*H(OH)-R1 (2) (B) leaving P1 from said amino alcohol derivative represented by formula (2) to synthesize an amino alcohol derivative represented by the following formula (3):R2-CH2-C*H(NH2)-C*H(OH)-R1 (3) (C) reacting said amino alcohol derivative represented by formula (3) with a carboxylic acid represented by R11COOH or a reactive derivative thereof to prepare a 2-acylamino alcohol derivative represented by the following formula (4):R2-CH2-C*H(NHCOR11)-C*H(OH)-R1 (4 ) wherein * represents an asymmetric carbon atom, and P1, R1, R2 and R11 are defined in the specification. A process for preparing alcohol derivatives having an acylamino group through several steps from amino group-protected 2-aminopropanol derivatives, and novel amino alcohols useful as intermediates in the process for preparing the alcohol derivative.

대표청구항 ▼

1. An amino alcohol derivative of formula (2):R2-CH2-(C*)H(NHP1)-(C*)H(OH)-R1 (2) wherein C* is an asymmetric carbon atom; P1 is an alkyl group having from 3 to 18 carbon atoms or an amino-protecting group selected from the group consisting of (i) a benzyloxycarbonyl group which may be substituted with a nitro group, a halogen atom, a lower alkoxyl group, a (lower alkoxyl)phenylazo group or a phenylazo group and (ii) an alkoxycarbonyl group having a straight, branched or cyclic alkyl group which may be substituted with a fluorenyl group or a methylsulfonyl group; R1 is an alkyl group, a cycloalkyl group or an aryl group; and R2 is [EQU5]wherein R3 and R4 are the same or different and each is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a hydroxyl-lower-alkyl group, a lower alkoxyalkyl group, an amino-lower-alkyl group, a cycloalkyl group, a hydroxycycloalkyl group, an aralkyl group or a piperazino group which may be substituted with a lower alkyl group; and when R3 and R4 each is a hydrogen atom; R7 is a lower alkylene group which may be discontinued by an oxygen atom; R8 and R9 are the same or different and each is a hydrogen atom, a lower alkyl group or a hydroxyl-lower-alkyl group, or R8 and R9 are together with a nitrogen atom to which each is bound, a piperidino group or a morpholino group, each of which may be substituted with a lower alkyl group; p is 2 or 3; and X is formula (VII) or (VIII): [EQU6]wherein R10 is a hydrogen atom, a lower alkyl group, an acyl group, a (lower alkoxyl)carbonyl group or a pyridyl group.

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[미국특허] Amino alcohol derivative and method for preparing the same 원문보기

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