Tổng hợp acefyllin dược dụng từ theophyllin

0 Người đánh giá. Xếp hạng trung bình 0

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:

Bộ sưu tập: Metadata

ID: 397176

Thêm vào giỏ Liên kết toàn văn

Theophyllin đã được sử dụng trong nhiều thập niên để trị bệnh hen suyễn cấp và mạn tính. Tuy nhiên, thực tế sử dụng theophyllin không hề dễ dàng. Theophyllin ít tan trong nước, gây khó chịu dạ dày và nhịp tim nhanh. Dẫn chất của theophyllin là acefyllin (theophyllin-7-acetic acid) có ít tác dụng phụ hơn. Acefyllin được tổng hợp bởi Baisse vào năm 1949[1] và hiện nay được dùng thay thế theophyllin, nhưng phải nhập từ nước ngoài. Do đó đề tài tham gia nghiên cứu tổng hợp acefyllin nhằm chủ động tạo nguồn nguyên liệu trong nước thay thế ngoại nhập. Phản ứng tổng hợp acefyllin được tiến hành ở nhiệt độ 90oC, tỉ lệ mol theophyllin: acid cloroacetic: NaOH = 1 : 1,6 : 2,9 cho hiệu suất cao. Sản phẩm được xác định cấu trúc bằng FTIR, MS, 1H NMR và 13C NMR, đạt độ tinh khiết cao 99,97% (HPLC) và có thể sử dụng làm nguyên liệu thuốc., 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.

1. Đọc trực tuyến

1. Đọc trực tuyến

Tạo bộ sưu tập với mã QR