Artabotrine 1 is a novel N-methoxylated 4,5-dioxoaporphine alkaloid which has been reported to be cytotoxic against P-388 cells. The total synthesis of 1 was carded out, and one of its analogue, N-methoxycepharadione ...Artabotrine 1 is a novel N-methoxylated 4,5-dioxoaporphine alkaloid which has been reported to be cytotoxic against P-388 cells. The total synthesis of 1 was carded out, and one of its analogue, N-methoxycepharadione B 2, was also synthesized. Both of the alkaloids and several intermediates were cytotoxic to several selected tumor cell lines.展开更多
Two new naphthoquinones, nocardione A and B isolated from strain P-A0248, were synthesized from naphtho[1,2-b]furan 1. The furan 1 was prepared from 5-methoxyl-1-naphthol.
Two series of novel compounds designed as hybrids of 1-arylnaphthalene lignans with dihydroisoquinolines or isoquinolines were synthesized and evaluated for their cytotoxicities on human tumor cell lines, such as A549...Two series of novel compounds designed as hybrids of 1-arylnaphthalene lignans with dihydroisoquinolines or isoquinolines were synthesized and evaluated for their cytotoxicities on human tumor cell lines, such as A549, Hela, PC-3 and KB. Some of the synthetic compounds exhibited their IC50 values on selected cell lines at μmol/L scale.展开更多
Reaction of simple dialkyl phosphites with symmetrical 1,3,5-trisubstituted hexahydro- triazines (HHTs) in the presence of benzyl chloride, afforded tertiaryaminomethylphosphonates in excellent yields. Glyphosate, a-...Reaction of simple dialkyl phosphites with symmetrical 1,3,5-trisubstituted hexahydro- triazines (HHTs) in the presence of benzyl chloride, afforded tertiaryaminomethylphosphonates in excellent yields. Glyphosate, a-aminomethylphosphonates and their derivatives can therefore be synthesized by this procedure conveniently.展开更多
A short and convergent approach for the synthesis of shikalkin （dl-shikonin） is presented. Stobbe reaction was employed to construct the aromatic skeleton 6. This is followed by a practical method to prepare the key...A short and convergent approach for the synthesis of shikalkin （dl-shikonin） is presented. Stobbe reaction was employed to construct the aromatic skeleton 6. This is followed by a practical method to prepare the key epoxides 9 from aldehydes 8 in high yield. Finally, shikalkin is achieved by Grignard reaction and oxidation.展开更多
A new facile route for the synthesis of dl-shikonin is presented. Reformatsky reaction assisted cross-coupling of 1, 4, 5, 8-tetramethoxynaphthalene-2-carbaldehyde and ethyl- bromoacetate was employed for introductio...A new facile route for the synthesis of dl-shikonin is presented. Reformatsky reaction assisted cross-coupling of 1, 4, 5, 8-tetramethoxynaphthalene-2-carbaldehyde and ethyl- bromoacetate was employed for introduction of the side chain of dl-shikonin.展开更多
3(R)-(t-Butyldiphenylsilyloxy)-1-penten-4-yne was prepared using D-xylose as the chiral template via an improved procedure for aldehyde-to-alkyne homologation in high yield.
In our effort to asymmetric synthesis of R-(+)-shikonin,a novel acetyl migration was found,and the mechanism of the migration was considered to be mediated by a 6 atom-ring intermediate.
文摘Artabotrine 1 is a novel N-methoxylated 4,5-dioxoaporphine alkaloid which has been reported to be cytotoxic against P-388 cells. The total synthesis of 1 was carded out, and one of its analogue, N-methoxycepharadione B 2, was also synthesized. Both of the alkaloids and several intermediates were cytotoxic to several selected tumor cell lines.
基金We thank theNationalNaturalScienceFoundation ofChina[20002005] for financial supports.
文摘Two new naphthoquinones, nocardione A and B isolated from strain P-A0248, were synthesized from naphtho[1,2-b]furan 1. The furan 1 was prepared from 5-methoxyl-1-naphthol.
文摘Two series of novel compounds designed as hybrids of 1-arylnaphthalene lignans with dihydroisoquinolines or isoquinolines were synthesized and evaluated for their cytotoxicities on human tumor cell lines, such as A549, Hela, PC-3 and KB. Some of the synthetic compounds exhibited their IC50 values on selected cell lines at μmol/L scale.
文摘Reaction of simple dialkyl phosphites with symmetrical 1,3,5-trisubstituted hexahydro- triazines (HHTs) in the presence of benzyl chloride, afforded tertiaryaminomethylphosphonates in excellent yields. Glyphosate, a-aminomethylphosphonates and their derivatives can therefore be synthesized by this procedure conveniently.
文摘A short and convergent approach for the synthesis of shikalkin （dl-shikonin） is presented. Stobbe reaction was employed to construct the aromatic skeleton 6. This is followed by a practical method to prepare the key epoxides 9 from aldehydes 8 in high yield. Finally, shikalkin is achieved by Grignard reaction and oxidation.
文摘A new facile route for the synthesis of dl-shikonin is presented. Reformatsky reaction assisted cross-coupling of 1, 4, 5, 8-tetramethoxynaphthalene-2-carbaldehyde and ethyl- bromoacetate was employed for introduction of the side chain of dl-shikonin.
基金the State Key Laboratory of Drug Research for the financial support.
文摘3(R)-(t-Butyldiphenylsilyloxy)-1-penten-4-yne was prepared using D-xylose as the chiral template via an improved procedure for aldehyde-to-alkyne homologation in high yield.
文摘In our effort to asymmetric synthesis of R-(+)-shikonin,a novel acetyl migration was found,and the mechanism of the migration was considered to be mediated by a 6 atom-ring intermediate.
