描述了合成衍生自伯芳族胺的N,O-缩醛的一般方法。已经研究了这些化合物在中性和酸性条件下的反应性,可以将标题化合物设想为通用的H 2 C NAr或(H 2 C NHAr)+等同物。在控制pH的酸性介质中加热时,N,O-氨基缩醛已通过适度加热分别转化为过氢三嗪和双(4-氨基芳基)甲烷衍生物或N-苄基芳基胺。的还原Ñ,ö-乙缩醛与氰基硼氢化钠的作用表明,C-O键仅在酸性介质中被破坏。
描述了合成衍生自伯芳族胺的N,O-缩醛的一般方法。已经研究了这些化合物在中性和酸性条件下的反应性,可以将标题化合物设想为通用的H 2 C NAr或(H 2 C NHAr)+等同物。在控制pH的酸性介质中加热时,N,O-氨基缩醛已通过适度加热分别转化为过氢三嗪和双(4-氨基芳基)甲烷衍生物或N-苄基芳基胺。的还原Ñ,ö-乙缩醛与氰基硼氢化钠的作用表明,C-O键仅在酸性介质中被破坏。
Monoalkylation of primary aromatic amines via N-(alkoxymethyl)aryl amines. Evidence for the formation of stable monomeric methyleneamines
作者:José Barluenga、Ana M. Bayón、Gregorio Asensio
DOI:10.1039/c39830001109
日期:——
Monomericmethyleneamines (1), formed from N-(alkoxymethyl)arylamines (3), are stable at –60 °C and may be trapped with organometallic reagents to provide the N-alkylarylamines (7).
The present invention provides 2-aminoquinazoline derivatives represented by formula (I):
wherein R1 and R2 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like;
X represents a bond or CR7aR7b wherein R7a and R7b may be the same or different and each represents a hydrogen atom, and the like;
when X is a bond, R3 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group;
when X is CR7aR7b wherein R7a and R7b have the same meanings as defined above, respectively, R3 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, and the like;
R4 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, and the like; and
R5 represents a hydrogen atom, substituted or unsubstituted aryl, and the like, or a pharmaceutically acceptable salt thereof.
A new synthesis of aziridine-2-carboxylates: Reaction of hexahydro-1,3,5-triazines or N-methoxymethylanilines with alkyl diazoacetates in the presence of lewis acid
作者:Hyun-Joon Ha、Jang-Min Suh、Kyung-Ho Kang、Young-Gil Ahn、Oksoo Han
DOI:10.1016/s0040-4020(97)10358-1
日期:1998.1
Aziridine-2-carboxylates were prepared from the reaction of hexahydro-1,3,5-triazines or N-methoxymethylanilines with alkyl diazoacetates in the presence of Lewis acid catalyst in high yield. (C) 1997 Elsevier Science Ltd. All rights reserved.
Ha, Hyun-Joon; Ahn, Young-Gil; Chon, Jung-Kyoon, Journal of the Chemical Society. Perkin transactions I, 1995, # 20, p. 2631 - 2634
作者:Ha, Hyun-Joon、Ahn, Young-Gil、Chon, Jung-Kyoon
DOI:——
日期:——
Addition of 1-Boc-2-tert-butyldimethylsilyloxypyrrole to N-Methyleneamine Equivalents: Synthesis of 1-Boc-5-aminomethyl-2,5-dihydropyrrol-2-ones and 1-Boc-2-oxo-1,7,9-triazaspiro[4,5]dec-3-enes
N-Methyleneamine equivalents generated from 1,3,5-triphenylhexahydro-1,3,5-triazines or N-methoxymethylanilines reacted with 1-Boc-2-tert-butyldimethylsilyloxypyrrole to give 1-Boc-5-anilinomethyl-2,5-dihydropyrrol-2-ones. However, the same reaction from 1,3,5-trialkylhexahydro-1,3,5-triazines yielded unexpected product of 1-Boc-7,9-dialkyl-2-oxo-1,7,9-triazaspiro[4,5]dec-3-enes.