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A kind of synthetic method of penicillin g sulfoxide benzhydryl ester

A technology of diphenylmethyl sulfoxide and synthesis method, applied in the direction of organic chemistry, etc., can solve the problems of peracetic acid flammability, low safety factor, unfavorable operation, etc., achieve effective non-chlorine oxidation ability, high safety factor, easy The effect of the operation

Active Publication Date: 2022-06-21
YANCHENG KAIYUAN MEDICINE CHEM
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there are two main aspects to the research on the oxidation process of penicillin G sulfoxide benzhydryl ester. One is to adopt the peracetic acid method, which has a high yield, but produces a large amount of acidic waste water, and the pollution is relatively serious, and the synthesis of peracetic acid belongs to High-risk process, peracetic acid is flammable, explosive, highly corrosive, and highly irritating, which is not conducive to operation and has a low safety factor; the second is to use hydrogen peroxide and supported catalyst oxidation method, which has low yield

Method used

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  • A kind of synthetic method of penicillin g sulfoxide benzhydryl ester
  • A kind of synthetic method of penicillin g sulfoxide benzhydryl ester
  • A kind of synthetic method of penicillin g sulfoxide benzhydryl ester

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Embodiment 1

[0028] (1) Synthesis of compound 2:

[0029] In a 500ml four-necked flask, add 120ml of dichloromethane, benzyl alcohol (23.2g, 0.126mol), compound 1 (40g, 0.107mol) and cool down to 15°C, add pyridine (16g, 0.202mol), and control the temperature for 10-15 ℃ Methylsulfonyl chloride (16 g, 0.140 mol) was added dropwise, controlled to finish dropping for 60 min, and the temperature was kept for 4 hours after the dropping. After the insulation was completed, 135 g of 5% dilute sulfuric acid was added for washing, the organic phase was separated, the aqueous phase was extracted with 30 ml of dichloromethane, and the organic phases were combined to obtain a dichloromethane solution of compound 2, which was transferred to a 1000 ml four-necked flask for use.

[0030] (2) Synthesis of compound 3:

[0031] The dichloromethane solution of compound 2 prepared in the previous step was adjusted to a temperature of 22°C. Preparation of potassium hydrogen persulfate complex salt aqueous s...

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Abstract

The invention discloses a synthesis method of penicillin G sulfoxide benzhydryl ester. Using penicillin G potassium salt as the starting material, first esterification, and then 2KHSO 5 ·KHSO 4 ·K 2 SO 4 The oxidative synthesis of penicillin G sulfoxide benzhydryl ester has a product purity of more than 99% and a total molar yield of more than 95%, and is suitable for industrial production. The invention has the advantages of readily available raw materials, high yield, less pollution, high safety factor, easy operation and the like.

Description

technical field [0001] The invention belongs to the field of synthesis of small molecular compounds, and relates to a method for synthesizing penicillin G sulfoxide diphenyl methyl ester. Background technique [0002] Cephalosporins are an important class of antibiotics. They have strong antibacterial effect, good curative effect and low toxicity. They have the dual properties of broad-spectrum and anti-penicillinase. Therefore, it has a very broad development prospect as a clinical first-line drug. At present, cephalosporins and their intermediates such as 7-AVCA, 7-ACCA, 7-ANCA and 7-AMCA are mainly prepared from 7-ACA and penicillin. However, due to the high preparation cost of 7-ACA as a raw material [1], many people turn their attention to penicillin raw materials with a wide range of sources and relatively cheap prices. Penicillin G sulfoxide diphenyl methyl ester is an important intermediate in the synthesis of cephalosporins, and the research on its synthesis proce...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D499/46C07D499/04
CPCC07D499/46C07D499/04
Inventor 邱国华陈迪才汪前胜王红萍
Owner YANCHENG KAIYUAN MEDICINE CHEM
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