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A rapid, high-yield conversion of codeine to morphine

Journal of Medicinal Chemistry

|January 1, 1977

Summary

This summary is machine-generated.

Boron tribromide efficiently converts codeine to morphine in high yields. This simple method offers a superior alternative for morphine synthesis and isolation.

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Area of Science:

Organic Chemistry
Medicinal Chemistry

Background:

Codeine is an opiate analgesic and a precursor in the synthesis of other opioids.
Existing methods for converting codeine to morphine can be complex and yield-limited.

Purpose of the Study:

To develop a more efficient and simpler method for the demethylation of codeine to morphine.
To establish a high-yielding synthetic route for morphine production.

Main Methods:

Treatment of codeine with boron tribromide in chloroform.
Simple isolation procedure following the reaction.

Main Results:

Consistent yields of morphine between 90-91% were achieved.
The reaction and isolation process were found to be operationally simple.

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Conclusions:

Boron tribromide is a highly effective reagent for the efficient conversion of codeine to morphine.
This method presents a significant improvement over previously reported procedures in terms of yield and simplicity.