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作者曾报导了四圜素和脫水四圜素的合成途径。我們拟定的另一合成金霉素及脫水金霉素的途径是从2-氯5-甲氧基苯乙酮(Ⅰ)的Stobbe縮合开始。以所获得的β-乙氧羰基-γ-(2-氯-5-甲氧基-苯基)Δ~(β,γ)戊烯酸(Ⅱ)环化成β-萘甲酸的衍生物后,还原为醛(Ⅲ),再經一次Stobbe或Perkin縮合或其它反应,氢化,环化后可期获得(Ⅳ),然后再构造A环。显然,从(Ⅳ)合成脱二甲胺脱羟脱水金霉素(Ⅴ)不过是一般常規实驗而已。至于合成金霉素本身则可先将(Ⅱ)內酯化,破环后可期获得烷氧基酸(Ⅵ),經上述一系列步驟,最后可期获得金霉素。
The authors have reported the synthesis of tetracene and dehydrated tetracene. The other route we have developed for the synthesis of Chlortetracycline and Dehydrated Chlortetracycline begins with the Stobbe condensation of 2-chloro-5-methoxyacetophenone (I). After the cyclization of β-naphthoic acid derivative with β-ethoxycarbonyl-γ- (2-chloro-5-methoxy-phenyl) Δ ~ (β, γ) Reduction to aldehyde (Ⅲ), followed by a Stobbe or Perkin condensation or other reactions, hydrogenation, cyclization can be obtained (Ⅳ), and then A ring structure. Obviously, the synthesis of desferrioxamine (V) from (IV) is nothing more than a routine experiment. As for the synthesis of chlortetracycline itself can be the first (Ⅱ) lactonization, broken ring after the availability of alkoxy acid (Ⅵ), after the above series of steps, the last period can be obtained chlortetracycline.