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首页> 外文期刊>Journal of health science. >Preparation of Metabolites by Chemical Reaction: Conversion of Antipsychotic Phenothiazines to their Sulfoxides and Tertiary Ami no Cyclic Antidepressants to their N-Oxide with Hydrogen Peroxide Using Titanosilicate Catalyst
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Preparation of Metabolites by Chemical Reaction: Conversion of Antipsychotic Phenothiazines to their Sulfoxides and Tertiary Ami no Cyclic Antidepressants to their N-Oxide with Hydrogen Peroxide Using Titanosilicate Catalyst

机译：通过化学反应制备代谢物：使用钛白硅酸盐催化剂将过氧化氢将抗精神病药物吩噻嗪转化为亚砜，将叔胺类环状抗抑郁剂转化为N-氧化物

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The aim of this study was to establish a preparation method needed to analyze the metabolites of an analytical procedure for antipsychotic phenothiazines and tertiary amino cyclic antidepressants by chemical reaction. These drugs were oxidized to their sulfoxide and N-oxide, respectively, with hydrogen peroxide using titanosilicate as the catalyst. An acidic medium (pH 3.0) containing 20% methanol was found to be optimal for the preparation of phenothiazine sulfoxide, and an alkaline medium (pH 10.5) containing 50% methanol was optimal for the preparation of the N-oxide of tertiary amino cyclic antidepressants. Each preparative scale reaction (2 mmol) was carried out and the crystallized product of each oxide was obtained. The amount of hydrogen peroxide needed to obtain the best yields of sulfoxide was 1.3-2.0 times the molar equivalent of the phenothiazines. The purities of the prepared crystallized product of the phenothiazine sulfoxides were good except for periciazine sulfoxide. The amounts of hydrogen peroxide needed to obtain the best yields of N-oxide were 4-5 times the molar equivalent of tertiany amino cyclic antidepressants. The purities of the crystals of each N-oxide were 99.5-100%. The characteristic mass fragment ions of each prepared oxide that were distinguishable as the N-oxides from parent drug could be confirmed when the collisional energy was decreased to 10 eV. ~1H- and ~(13)C-NMR spectral data confirmed the structure of the prepared mianserin N-oxide to be 2-oxide. In conclusion, a simple and rapid preparation method for oxide metabolites of phenothiazines and tertiary amino cyclic antidepressants available as analytical standards was established.
机译：这项研究的目的是建立一种通过化学反应分析抗精神病性吩噻嗪和叔氨基环抗抑郁药的分析方法代谢物所需的制备方法。使用钛硅酸盐作为催化剂，用过氧化氢将这些药物分别氧化为亚砜和N-氧化物。发现含有20％甲醇的酸性介质（pH 3.0）最适合制备吩噻嗪亚砜，含有50％甲醇的碱性介质（pH 10.5）最适于制备叔氨基环状抗抑郁药的N-氧化物。进行每种制备性规模的反应（2mmol），并且获得每种氧化物的结晶产物。获得最佳亚砜收率所需的过氧化氢量为吩噻嗪的摩尔当量的1.3-2.0倍。制备的吩噻嗪亚砜结晶产物的纯度好，除了哌嗪嗪亚砜以外。获得最佳N-氧化物收率所需的过氧化氢量是叔氨基环状抗抑郁药摩尔当量的4-5倍。每种N-氧化物的晶体纯度为99.5-100％。当碰撞能量降低到10 eV时，可以确认每种制备的氧化物的特征性质量碎片离子，这些离子可以与母药区别为N-氧化物。 〜1H-和〜（13）C-NMR光谱数据证实了所制备的棉酚素N-氧化物的结构为2-氧化物。总之，建立了一种简单快速的制备吩噻嗪类氧化物代谢物和叔氨基环抗抑郁药的方法，作为分析标准品。

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