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Process for preparing (cycloheptylamino) methylene biphosphonic acid

A technology of methylene diphosphonic acid and heptyl amino group is applied in the field of preparation of western medicine compounds, which can solve the problems of reaction control and product purification effect, and achieve the effects of low cost, high yield and mild reaction conditions.

Inactive Publication Date: 2002-08-14
深圳市资福药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although this method has advantages, it must first undergo an intermediate reaction to obtain the intermediate product N-cycloheptyl formamide, which will definitely have some impact on reaction control and product purification.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Add 56.6g (0.5mol) of cycloheptylamine, 81.5g (0.55mol) of triethyl orthoformate, and 218.6g (1.05mol) of triisopropyl phosphite into the reaction flask, heat to reflux for 2 hours, and remove the low boiling Add 300ml of hydrochloric acid, reflux for 1 hour, add methanol-acetone mixed solution after concentration, precipitate crystals, dry, product mp231-233°C, yield 85.0%.

Embodiment 2

[0019] By the same method as in Example 1, but replacing triisopropyl phosphite with triethyl phosphite, the yield was 75.1%.

Embodiment 3

[0021] By the same method as in Example 1, but replacing triethyl orthoformate with trimethyl orthoformate, the yield was 56.8%. 1. Elemental analysis (C 8 h 19 NO 6 P 2 )

[0022] CHN Calculated value (%) 33.46 6.67 4.87 Measured value (%) 33.21 7.02 4.742. Mass spectrum (FAB): 288 (M + +H, 70%) 3. Infrared spectrum (IR): 3421 (N-H), 2956, 2867 (C-H) 4. 1 H NMR spectrum ( 1 H-NMR): D 2 O is the solvent δ1.50-1.75, 10H (2Hc, 4Hd, 4He) δ2.11-2.15, 2H (2Hc) δ3.58, 1H (Hb) δ3.69, 1H (Ha)

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PUM

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Abstract

A process for preparing (cycloheptylamino methylene biphosphonic acid as bone absorption inhibitor is prepared through reacting trialkyl phosphite on cycloheptylamine and trialkyl orthoformate, adding hydrochloric acid and hydrolyzing. Its advantages include gentle reaction condition and simple operation.

Description

technical field [0001] The invention belongs to a preparation method of western medicine compounds, in particular to a preparation method of bisphosphonic acid bone resorption inhibitor (cycloheptylamino) methylene diphosphonic acid. Background technique [0002] Osteoporosis (Osteoposis) is a kind of multiple disease that seriously threatens human health, and our country has listed it as one of the three senile diseases that are focused on. As bone resorption inhibitors, bisphosphonic acid drugs have a strong affinity for calcium phosphate, and the amount required to inhibit the absorption of hydroxyapatite crystals is much lower than that required to inhibit the formation and growth, so a small dose can inhibit bone resorption And produce curative effect. Bisphosphonic acid drugs have been developed rapidly at home and abroad in recent years. They are not only used in the prevention and treatment of osteoporosis, but also in the treatment of hypercalcemia complicated by m...

Claims

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Application Information

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IPC IPC(8): C07F9/38
Inventor 谢敏浩罗世能何拥军邹霈刘娅灵
Owner 深圳市资福药业有限公司
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