Dynamic kinetic resolution method of 1-(1-naphthyl) ethylamine

A technology of dynamic kinetics and ethylamine, applied in the field of dynamic kinetics splitting of 1-ethylamine, can solve the problems of expensive resolving agent, many product side reactions, slow reaction rate, etc. The effect of high purity, fast reaction rate and great application value
CN102392065AInactive Publication Date: 2012-03-28ZHEJIANG UNIV
1 Cites 12 Cited by

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG UNIV
Publication Date
2012-03-28
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
Patent Text Reader

Abstract

The invention discloses a dynamic kinetic resolution method for 1-(1-naphthyl) ethylamine, which comprises the following steps of: firstly, adding parachlorophenol, organic acid, dicyclohexylcarbodiimide and 4-dimethylaminopyridine, carrying out agitating reaction and filtering, drying, concentrating and carrying out column chromatography to obtain an acyl donor; or adding acetophenone and sodium borohydride, carrying out agitating reaction, depressurizing and distilling, washing, extracting, drying and concentrating to obtain phenethyl alcohol, adding the phenethyl alcohol, acetyl chloride and triethylamine, carrying out agitating reaction and washing, drying, concentrating and carrying out column chromatography to obtain an acyl donor; secondly, adding palladium salt and a carrier, heating, adding formaldehyde and sodium hydroxide, heating and centrifuging, washing and vacuum-drying to obtain a racemic catalyst for standby; and thirdly, adding the 1-(1-naphthyl) ethylamine in methyl benzene, the acyl donor, lipase and the racemic catalyst and carrying out hydrogenation reaction to obtain amide. The dynamic kinetic resolution method has high reaction speed, lower temperature, high conversion rate and product optical purity and great application value.
Need to check novelty before this filing date? Find Prior Art

Description

field of invention

[0001] The invention relates to a dynamic kinetic resolution method, in particular to a dynamic kinetic resolution method for 1-(1-naphthyl)ethylamine. Background technique

[0002] Cinacalcet hydrochloride, chemical name (α R )-α-Methyl- N -[3-[3-(Trifluoromethyl)phenyl]propyl]-1-naphthylmethylamine hydrochloride, the first drug in a new class of compounds known as calcimimetics, capable of Activates calcium receptors in the parathyroid glands, thereby reducing parathyroid hormone (PTH) secretion. First launched in the United States in 2004, it is clinically used to treat hypercalcemia in patients with secondary hyperparathyroidism and parathyroid tumors caused by chronic kidney disease receiving dialysis. It can inhibit the secretion of parathyroid hormone by activating calcium ion receptors. It is well absorbed in the body and has good bioavailability (about 80%). It reaches the maximum blood concentration 3 hours after taking it, and it has long-ter...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More