KR930016404A - N-5-보호된 2,5-디아미노-4,6-디클로로 피리미딘 및 그의 제조방법 - Google Patents

N-5-보호된 2,5-디아미노-4,6-디클로로 피리미딘 및 그의 제조방법 Download PDF

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KR930016404A
KR930016404A KR1019930000799A KR930000799A KR930016404A KR 930016404 A KR930016404 A KR 930016404A KR 1019930000799 A KR1019930000799 A KR 1019930000799A KR 930000799 A KR930000799 A KR 930000799A KR 930016404 A KR930016404 A KR 930016404A
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South Korea
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protected
diamino
pyrimidine
dichloro
alkoxy
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KR1019930000799A
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English (en)
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KR100262283B1 (ko
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스투키 게르하드
프레비돌리 펠릭스
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하인즈 모제르, 비트 라우베르
론자 리미티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/30—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms

Abstract

본 발명은 항바이러스 성질을 가지는 의약품을 제조하는 중요한 중간 생성물인 일반 구조식 Ⅰ의 N-5-보호된 2,5-디아미노-4,6-디클로로피리미딘 및 그의 제조방법에 관한 것으로,
상기의 화합물은 N-보호된 아미노말론산 에스테르를 알콕시알칼리 존재하에 구아니딘과 함께 고리화시키고, 여기서 생성된 N-보호된-4,6-디하이드록시-2,5-디아미노 피리미딘을 염소치환하여 얻어지는 N-5-보호된-2,5-디아미노-4,6-디클로로 피리미딘 및 그의 제조방법.

Description

N-5-보호된 2,5-디아미노-4,6-디클로로 피리미딘 및 그의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. 아래의 일반적 구조를 가지고,
    R은 알콕시 또는 삼불화메틸기 의미하는 N-5-보호된 2,5-디아미노-4,6-디클로로 피리미딘.
  2. N-5-보호된 2,5-디아미노-4,6-디클로로피리미딘의 제조 방법에 있어서, R1이 C-C4의 저급알킬그룹인 아래의 일반 구조식 Ⅱ의 N-5 보호된 아미노말론산 에스테르는,
    알콕시 알칼리존재하에 구아니딘과 반응하여 아래 일반구조식 Ⅲ의 N-5-보호된-4,6-디하이드록시-2,5-디아미노 피리미딘으로,
    고리를 형성하고 구조식 Ⅲ의 피리미딘은 다시 포스포르옥시클로리드 최종생성물로 제조된 것을 특징으로 하는 N-5-보호된-2,5-디아미노-4,6-디클로로 피리미딘의 제조방법.
  3. 제2항에 있어서, N-보호된 아미노말론산 에스테르의 고리형성은 메탄을 용매에서 메톡시나트륨 또는 에탄올 용매에서 에톡시나트륨의 존재하에 상온에서 해당용매의 끓는 온도사이에서 숙행되어 진 것을 특징으로 하는 N-5-보호된-2,5-디아미노-4,6-디클로로 피리미딘의 제조방법.
  4. 제2항 또는 제3항에 있어서, 염소화반응은 80℃에서 포스포르옥시클로리드의 끓는 온도 사이에서 일어나는 것을 특징으로 하는 N-5-보호된-2,5-디아미노-4,6-디클로로 피리미딘의 제조방법.
  5. 제2항 내지 제4항중 어느 한 항에 있어서, 상기 제조의 공정에 사용되는 중간 생성물이고, R이 알콕시기 또는 삼불화메틸기인 아래의 일반적 구조 Ⅲ인 N-5-보호된-2,5-디아미노-4,6-디하이드록시 피리미딘,
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930000799A 1992-01-22 1993-01-21 N-5-보호된 2,5-디아미노-4,6-디클로로 피리미딘 및 그의 제조방법 KR100262283B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH17992 1992-01-22
CH179/92 1992-01-22

Publications (2)

Publication Number Publication Date
KR930016404A true KR930016404A (ko) 1993-08-26
KR100262283B1 KR100262283B1 (ko) 2000-08-01

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KR1019930000799A KR100262283B1 (ko) 1992-01-22 1993-01-21 N-5-보호된 2,5-디아미노-4,6-디클로로 피리미딘 및 그의 제조방법

Country Status (19)

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US (1) US5294710A (ko)
EP (1) EP0552758B1 (ko)
JP (1) JP3252502B2 (ko)
KR (1) KR100262283B1 (ko)
CN (1) CN1077193A (ko)
AT (1) ATE154346T1 (ko)
AU (1) AU658965B2 (ko)
CA (1) CA2087880C (ko)
CZ (1) CZ287049B6 (ko)
DE (1) DE59306703D1 (ko)
DK (1) DK0552758T3 (ko)
ES (1) ES2104966T3 (ko)
FI (1) FI930238A (ko)
HU (1) HU219231B (ko)
IL (2) IL104478A (ko)
MX (1) MX9300267A (ko)
PL (2) PL171743B1 (ko)
SK (1) SK279618B6 (ko)
ZA (1) ZA93431B (ko)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9402161D0 (en) * 1994-02-04 1994-03-30 Wellcome Found Chloropyrimidine intermediates
CA2145928C (en) * 1994-04-27 2007-10-09 Gerhard Stucky N-(2-amino-4,6-dichloropyrimidin-5-yl)formamide, and a process for its preparation
EP1188750B1 (de) * 1998-12-21 2003-10-15 Lonza AG Verfahren zur Herstellung von 2,5-Diamino-4,6-dihalogenpyrimidinen
US6608199B2 (en) * 2000-07-07 2003-08-19 Syngenta Limited Synthesis of chlorinated pyrimidines
CN102702110A (zh) * 2012-05-24 2012-10-03 盛世泰科生物医药技术(苏州)有限公司 一种4-氨基-5,6-二氯嘧啶的制备方法
CN103936681B (zh) * 2014-04-04 2015-07-29 苏州开元民生科技股份有限公司 2-氨基-4,6-二氯-5-甲酰胺基嘧啶的制备方法
CN117050024B (zh) * 2023-10-13 2024-01-05 苏州开元民生科技股份有限公司 一种2-氨基-4,6-二氯-5-甲酰胺基嘧啶的合成方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH649291A5 (de) * 1982-03-16 1985-05-15 Hoffmann La Roche Dicarbamate.
GB8916698D0 (en) * 1989-07-21 1989-09-06 Beecham Group Plc Novel process

Also Published As

Publication number Publication date
IL104478A0 (en) 1993-05-13
EP0552758A1 (de) 1993-07-28
ZA93431B (en) 1993-08-25
AU658965B2 (en) 1995-05-04
HUT63618A (en) 1993-09-28
FI930238A (fi) 1993-07-23
JPH05279344A (ja) 1993-10-26
CA2087880A1 (en) 1993-07-23
ATE154346T1 (de) 1997-06-15
SK393192A3 (en) 1995-09-13
ES2104966T3 (es) 1997-10-16
IL119700A0 (en) 1997-02-18
JP3252502B2 (ja) 2002-02-04
MX9300267A (es) 1993-11-01
PL171743B1 (pl) 1997-06-30
FI930238A0 (fi) 1993-01-21
KR100262283B1 (ko) 2000-08-01
CZ393192A3 (en) 1993-08-11
SK279618B6 (sk) 1999-01-11
EP0552758B1 (de) 1997-06-11
AU3200193A (en) 1993-07-29
PL171137B1 (pl) 1997-03-28
US5294710A (en) 1994-03-15
CA2087880C (en) 2004-06-15
CZ287049B6 (cs) 2000-08-16
HU9300182D0 (en) 1993-04-28
DK0552758T3 (da) 1997-07-07
CN1077193A (zh) 1993-10-13
IL104478A (en) 1997-06-10
HU219231B (en) 2001-03-28
DE59306703D1 (de) 1997-07-17
PL297517A1 (en) 1993-08-23

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