Tổng hợp acefyllin dược dụng từ theophyllin

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Tác giả: Linh Tý Huỳnh, Đào Thiện Nguyễn

Ngôn ngữ: Vie

Ký hiệu phân loại:

Thông tin xuất bản: Tạp chí khoa học và công nghệ - Đại học Nguyễn Tất Thành 2019

Mô tả vật lý: 49-54

Bộ sưu tập: Metadata

ID: 399631

Thêm vào giỏ Liên kết toàn văn

Theophylline đã được sử dụng trong nhiều thập kỷ để điều trị cả bệnh hen suyễn cấp tính và mãn tính. Tuy nhiên, trên thực tế, theophylline không phải là một loại thuốc đặc biệt dễ sử dụng vì các đặc tính vật lý và dược lý của nó. Nó hòa tan kém trong nước
hơn nữa, nó thường liên quan đến chứng khó chịu và đánh trống ngực. Một trong những dẫn xuất của theophylline đã được sử dụng để giảm tác dụng phụ là acefylline (axit theophylline-7-acetic). Acefylline được Baisse tổng hợp vào năm 1949 [1] và hiện được bán trên thị trường như một chất thay thế cho theophylline. Tuy nhiên, nguyên liệu sản xuất dược phẩm trong nước hiện nay chủ yếu phải nhập khẩu nên acefylline được tổng hợp. Hiệu suất tối ưu thu được khi phản ứng thực hiện ở 90oC, tỉ lệ mol theofylline: axit chloroacetic: NaOH = 1: 1,6: 2,9. Cấu trúc của nó đã được xác nhận bởi dữ liệu phổ FTIR, MS, 1H NMR và 13C NMR. Sản phẩm có tỷ lệ tinh khiết rất cao (99,97% theo HPLC) và có thể được sử dụng như một thành phần dược phẩm., Tóm tắt tiếng anh, Theophylline has been used for decades to treat both acute and chronic asthma. However, in practice, theophylline is not a particularly easy drug to use because of its physical and pharmacological properties. It is poorly soluble in water
furthemore, it is frequently associated with gatric upset and palpitations. One of the theophylline derivatives that has been used in an attempt to circumvent side effects is acefylline (theophylline-7-acetic acid). Acefylline was synthesized by Baisse in 1949[1] and is currently marketed as an alternative to theophylline. However, The raw material for domestic pharmaceutical production is now mainly imported, so acefylline was synthesized. The Optimal yield obtained when the reaction is carried out at 90oC, mol ratio theofylline: chloroacetic acid:NaOH = 1:1,6:2,9. Its structure was confirmed by FTIR, MS, 1H NMR and 13C NMR spectral data. The product has very high purity rate (99.97% by HPLC) and can be used as a pharmaceutical ingredient.

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