JPS5899472A - 25-hydroxyvitamin d3 26,33-lactol - Google Patents
25-hydroxyvitamin d3 26,33-lactolInfo
- Publication number
- JPS5899472A JPS5899472A JP19625381A JP19625381A JPS5899472A JP S5899472 A JPS5899472 A JP S5899472A JP 19625381 A JP19625381 A JP 19625381A JP 19625381 A JP19625381 A JP 19625381A JP S5899472 A JPS5899472 A JP S5899472A
- Authority
- JP
- Japan
- Prior art keywords
- hydroxyvitamin
- lactol
- formula
- aluminum hydride
- vitamin
- 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
Landscapes
- Furan Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
本発明は式（１）で示される２５−ヒドロキシビタミン
Ｄ３２６．２３−ラクトールに関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to 25-hydroxyvitamin D326.23-lactol represented by formula (1).
式（１）で示されるビタミンＤ３誘導体は新規化合物で
あり、例えば他用等の方法（Ｏｈｅｍ、 ＰｈａｒｚＢ
ｕｌｌ、ｅ２ｇ（９）、２８５２（１９８０））によっ
て得られる２５−ヒドロキシビタミンＤ３２６．２３−
ラクトンをトルエン等の不活性溶媒中水素化金属類例え
ばリチウム水素化アルミニウム、ジイソブチル水素化ア
ルミニウム（ＤＩＢＡＬ）等を用いて還元するととＫよ
り得られる。The vitamin D3 derivative represented by formula (1) is a new compound, and can be used, for example, by methods such as those used by others (Ohem, PharzB
25-hydroxyvitamin D326.23- obtained by Ull, e2g (9), 2852 (1980))
K is obtained by reducing the lactone with a metal hydride such as lithium aluminum hydride, diisobutyl aluminum hydride (DIBAL), etc. in an inert solvent such as toluene.
このようにして得られる本発明の化合物（１）はビタミ
ンＤ様の生物活性を有し医薬として有用である。The compound (1) of the present invention thus obtained has vitamin D-like biological activity and is useful as a medicine.
実施例。Example.
（１”） （Ｔり化合物（ｉ
ｔ）１．８Ｍｇをトルエン３００μＩＫ溶解し一７０℃
にてジイソブチル水素化アルミニウム（（ＤＩＢＡＬ）
の２５％ヘキサン溶液２６．５μｊ！を加え一７０℃で
２時間攪拌する。エタノール１５０μＬを加え過剰のＤ
ＩＢＡＬを分解後室温に戻しクロロホルムで希釈し５％
塩酸水で洗浄、億酸す） ＩＪウムで乾燥し溶媒を留去
すふ、残渣をセファデックｘＴ、Ｈ−２０Ｃｆｆｌ媒ク
ロロホルム、ヘキサン、メタノール、６５：３５：２）
を用いたカラムクロマトグラフィーに付し精製しく２３
８．２ＳＲ）−２５−ヒドロキシビタきンＤ３２６．２
３−ラクトール（１’） １．６７１１９を得る。(1”) (T compound (i
t) Dissolve 1.8Mg in toluene 300μIK and heat to -70℃
Diisobutyl aluminum hydride ((DIBAL)
26.5μj of 25% hexane solution! and stirred at -70°C for 2 hours. Add 150 μL of ethanol and remove excess D.
After decomposing IBAL, return to room temperature and dilute with chloroform to 5%
Wash with hydrochloric acid water, dilute with 100,000 ml of acid), dry with IJum, distill off the solvent, and dissolve the residue in Sephadec xT, H-20Cffl (chloroform, hexane, methanol, 65:35:2).
It was purified by column chromatography using 23
8.2SR)-25-Hydroxyvitanquin D326.2
3-lactol (1') 1.67119 is obtained.
−ｖＸ２ベクトル”／：４３０（Ｍ”）＃４１Ｌ３９４
１３７９．３５６，３４２，１３６，１１８’ＨＮＭＲ
Ｘベクトル（０ＤＯｊ！３） Ｊ ： ０．５５ （３
Ｈ，ｓ）。-vX2 vector”/:430(M”) #41L394
1379.356,342,136,118'HNMR
X vector (0DOj!3) J: 0.55 (3
H,s).
１．３４（３８，ｓ） 、３．８〜４．２（２Ｈ，惰）
、４．８３（２Ｈ，ｂｓ） 、５．０７（ＩＨ，ｂａ）
、６．１４（２Ｈ，ＡＢｑ。1.34 (38, s), 3.8~4.2 (2H, inertia)
, 4.83 (2H, bs), 5.07 (IH, ba)
, 6.14 (2H, ABq.
Ｊ−１１Ｈ１） ＵＶスペクトル：λ−（局方エタノール）２６５％Ｓ。J-11H1) UV spectrum: λ- (pharmacopoeial ethanol) 265% S.
１ｍ１％２２８ｓｓ 出願人 中外製薬株式会社1m1%228ss Applicant: Chugai Pharmaceutical Co., Ltd.
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP19625381A JPS5899472A (en) | 1981-12-08 | 1981-12-08 | 25-hydroxyvitamin d3 26,33-lactol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP19625381A JPS5899472A (en) | 1981-12-08 | 1981-12-08 | 25-hydroxyvitamin d3 26,33-lactol |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5899472A true JPS5899472A (en) | 1983-06-13 |
| JPH0261469B2 JPH0261469B2 (en) | 1990-12-20 |
Family
ID=16354728
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP19625381A Granted JPS5899472A (en) | 1981-12-08 | 1981-12-08 | 25-hydroxyvitamin d3 26,33-lactol |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5899472A (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH04118164U (en) * | 1991-03-29 | 1992-10-22 | タキロン株式会社 | fountain device |
-
1981
- 1981-12-08 JP JP19625381A patent/JPS5899472A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0261469B2 (en) | 1990-12-20 |
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