2,3-diphenylpropanoyl chloride -Drug Synthesis Database

【结构式】

【分子编号】29484

【品名】2,3-diphenylpropanoyl chloride

【CA登记号】

【分子式】C₁₅H₁₃ClO

【分子量】244.72032

【元素组成】C 73.62% H 5.35% Cl 14.49% O 6.54%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号：(IV)

The reaction of m-xylene-alpha,alpha'-diamine (I) with N,N'-bis(tert-butoxycarbonyl)pyrazole-1-carboxamidine (II) in THF gives the protected guanidine (III), which is acylated at the free amino group with 2,3-diphenylpropionyl chloride (IV) and triethylamine in dichloromethane affording the amide (V). The condensation of (V) with tetrahydrofuran-2-ylmethylamine (VI) in refluxing THF affords the protected amidinourea (VII), which is finally treated with TFA in dichloromethane.

参考文献中间体

合成目标

【1】 Biftu, T.; et al.; Synthesis and SAR of oxodiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents. 217th ACS Natl Meet (March 21 1999, Anaheim) 1999, Abst MEDI 138.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	19167	3-(aminomethyl)benzylamine; [3-(aminomethyl)phenyl]methanamine	1477-55-0	C₈H₁₂N₂	详情	详情
(II)	29482	N,N-bis-Boc-1-guanylpyrazole; tert-butyl (E)-[(tert-butoxycarbonyl)amino](1H-pyrazol-1-yl)methylidenecarbamate	152120-54-2	C₁₄H₂₂N₄O₄	详情	详情
(III)	29483	tert-butyl (Z)-[[3-(aminomethyl)benzyl]amino][(tert-butoxycarbonyl)amino]methylidenecarbamate		C₁₉H₃₀N₄O₄	详情	详情
(IV)	29484	2,3-diphenylpropanoyl chloride		C₁₅H₁₃ClO	详情	详情
(V)	29485	tert-butyl (Z)-[(tert-butoxycarbonyl)amino][(3-[[(2,3-diphenylpropanoyl)amino]methyl]benzyl)amino]methylidenecarbamate		C₃₄H₄₂N₄O₅	详情	详情
(VI)	27335	Tetrahydro-2-furanylmethanamine; Tetrahydrofurfurylamine	4795-29-3	C₅H₁₁NO	详情	详情
(VII)	29486	tert-butyl (Z)-[(3-[[(2,3-diphenylpropanoyl)amino]methyl]benzyl)amino]([[(tetrahydro-2-furanylmethyl)amino]carbonyl]amino)methylidenecarbamate		C₃₅H₄₃N₅O₅	详情	详情

Extended Information