JP2000503975A - プリン誘導体の製造方法 - Google Patents
プリン誘導体の製造方法Info
- Publication number
- JP2000503975A JP2000503975A JP9526505A JP52650597A JP2000503975A JP 2000503975 A JP2000503975 A JP 2000503975A JP 9526505 A JP9526505 A JP 9526505A JP 52650597 A JP52650597 A JP 52650597A JP 2000503975 A JP2000503975 A JP 2000503975A
- Authority
- JP
- Japan
- Prior art keywords
- amino
- acid
- valine
- group
- dihydro
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.化合物2−(2−アミノ−1,6−ジヒドロ−6−オキソ−プリン−9−イ ル)−メトキシ−3−ヒドロキシ−1−プロピル−L−バリナート又はその薬学 的に許容できる塩又はそのジアステレオマーの製造方法であって、 (a)2−(2−アミノ−1,6−ジヒドロ−6−オキソ−プリン−9−イル) −メトキシ-1,3−プロパンジイル−ビス−L−バリナート又はその塩を、低 級アルキルアミン、ベンジルアミン又はベンジルメチルアミンで部分的に加水分 解して、化合物2−(2−アミノ−1,6−ジヒドロ−6−オキソ−プリン−9 −イル)−メトキシ−3−ヒドロキシ−1−プロピル−L−バリナート又はその 薬学的に許容される塩を得ること: (b)場合により、式: (式中、P1は、水素又はアミノ−保護基であり、P2は、アミノ−保護基である ) を有する化合物からアミノ保護基を除去して、化合物2−(2−アミノ−1,6 −ジヒドロ−6−オキソ−プリン−9−イル)−メトキシ−3−ヒドロキシ−1 −プロピル−L−バリナート又はその薬学的に許容される塩を得ること; (c)場合により、化合物2−(2−アミノ−1,6−ジヒドロ−6−オキソ− プリン−9−イル)−メトキシ-3−ヒドロキシ−1−プロピル−L−バリナー トをその薬学的に許容される塩に転化すること; (d)場合により、化合物2−(2−アミノ−1,6−ジヒドロ−6−オキソ− プリン−9−イル)−メトキシ−3−ヒドロキシ−1−プロピル−L−バリナー トの酸付加塩を非塩型に転化すること;又は、 (e)場合により、2−(2−アミノ−1,6−ジヒドロ−6−オキソ−プリン − 9−イル)−メトキシ−3−ヒドロキシ−1−プロピル−L−バリナートをその (R)及び(S)ジアステレオ異性体に分割すること、 のいずれか一つ又はその組み合わせを含む方法。 2.該低級アルキルアミンが、n−プロピルアミンである請求項1記載の方法。 3.該加水分解が、非極性非プロトン溶媒中で、好ましくはヘキサン中で行われ る請求項1記載の方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US592,080 | 1996-01-26 | ||
US08/592,080 US5700936A (en) | 1996-01-26 | 1996-01-26 | Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol valinate |
PCT/EP1997/000229 WO1997027195A1 (en) | 1996-01-26 | 1997-01-18 | Process for preparing purine derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2000503975A true JP2000503975A (ja) | 2000-04-04 |
JP4091115B2 JP4091115B2 (ja) | 2008-05-28 |
Family
ID=24369201
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP52650597A Expired - Lifetime JP4091115B2 (ja) | 1996-01-26 | 1997-01-18 | プリン誘導体の製造方法 |
Country Status (7)
Country | Link |
---|---|
US (1) | US5700936A (ja) |
EP (1) | EP0877746B1 (ja) |
JP (1) | JP4091115B2 (ja) |
AU (1) | AU1592997A (ja) |
DE (1) | DE69706828T2 (ja) |
ES (1) | ES2163117T3 (ja) |
WO (1) | WO1997027195A1 (ja) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6703394B2 (en) | 1996-02-16 | 2004-03-09 | Medivir Ab | Acyclic nucleoside derivatives |
US5869493A (en) * | 1996-02-16 | 1999-02-09 | Medivir Ab | Acyclic nucleoside derivatives |
CN1860120A (zh) * | 2003-08-28 | 2006-11-08 | 兰贝克赛实验室有限公司 | 无定形盐酸缬更昔洛韦 |
WO2005092891A2 (en) * | 2004-03-29 | 2005-10-06 | Ranbaxy Laboratories Limited | Preparation of esters of ganciclovir |
ZA200702234B (en) * | 2006-03-21 | 2008-07-30 | Cipla Ltd | Preparation of ester of purine derivatives |
EP1870411B1 (en) * | 2006-06-21 | 2016-03-16 | Fidia Farmaceutici S.p.A. | Process for the preparation and purification of valgancyclovir |
US20090076040A1 (en) * | 2007-09-15 | 2009-03-19 | Protia, Llc | Deuterium-enriched valganciclovir |
WO2010036904A2 (en) * | 2008-09-26 | 2010-04-01 | Dr. Reddy's Laboratories Ltd. | Preparation of valganciclovir and its salts |
CN102070635B (zh) * | 2009-11-19 | 2013-01-30 | 浙江车头制药股份有限公司 | 一种更昔洛韦缬氨酸酯衍生物的制备方法 |
US20110207931A1 (en) * | 2010-02-23 | 2011-08-25 | Srinivas Katkam | Preparation of valganciclovir and its salts |
EP2714691B1 (en) | 2011-05-31 | 2016-09-07 | Pharmathen S.A. | Process for the preparation of 2-amino-9-((2-phenyl-1,3-dioxan-5-yloxy)methyl)-1h-purin-6(9h)-one compound useful in the preparation of valganciclovir |
CN111763207B (zh) * | 2019-04-02 | 2024-05-10 | 北京万全德众医药生物技术有限公司 | 一种盐酸缬更昔洛韦的制备方法 |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1523865A (en) * | 1974-09-02 | 1978-09-06 | Wellcome Found | Purine compunds and salts thereof |
US4355032B2 (en) * | 1981-05-21 | 1990-10-30 | 9-(1,3-dihydroxy-2-propoxymethyl)guanine as antiviral agent | |
DE3278501D1 (en) * | 1981-08-11 | 1988-06-23 | Wellcome Found | Antiviral compounds |
NL8202626A (nl) * | 1982-06-29 | 1984-01-16 | Stichting Rega V Z W | Derivaten van 9-(2-hydroxyethoxymethyl)guanine. |
JPS5989682A (ja) * | 1982-10-14 | 1984-05-23 | ザ・ウエルカム・フアウンデ−シヨン | プリン誘導体 |
AP55A (en) * | 1987-08-15 | 1989-09-26 | The Wellcome Foundation Ltd | Therapeutic Acyclic Nucleosides |
CA2005815C (en) * | 1988-12-19 | 1999-08-03 | Wellcome Foundation Limited (The) | Antiviral acyclic nucleoside derivatives |
ES2157259T3 (es) * | 1993-06-10 | 2001-08-16 | Rolabo Sl | Procedimiento para preparar esteres de aminoacidos y analogos de nucleosidos. |
PE32296A1 (es) * | 1994-07-28 | 1996-08-07 | Hoffmann La Roche | Ester de l-monovalina derivado de 2-(2-amino-1,6-dihidro-6-oxo-purin-9-il) metoxi-1,3-propandiol y sus sales farmaceuticamente aceptables |
-
1996
- 1996-01-26 US US08/592,080 patent/US5700936A/en not_active Expired - Lifetime
-
1997
- 1997-01-18 EP EP97902185A patent/EP0877746B1/en not_active Expired - Lifetime
- 1997-01-18 DE DE69706828T patent/DE69706828T2/de not_active Expired - Lifetime
- 1997-01-18 JP JP52650597A patent/JP4091115B2/ja not_active Expired - Lifetime
- 1997-01-18 ES ES97902185T patent/ES2163117T3/es not_active Expired - Lifetime
- 1997-01-18 WO PCT/EP1997/000229 patent/WO1997027195A1/en active IP Right Grant
- 1997-01-18 AU AU15929/97A patent/AU1592997A/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
EP0877746A1 (en) | 1998-11-18 |
US5700936A (en) | 1997-12-23 |
DE69706828T2 (de) | 2002-04-04 |
ES2163117T3 (es) | 2002-01-16 |
EP0877746B1 (en) | 2001-09-19 |
WO1997027195A1 (en) | 1997-07-31 |
AU1592997A (en) | 1997-08-20 |
DE69706828D1 (de) | 2001-10-25 |
JP4091115B2 (ja) | 2008-05-28 |
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