TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
批准号:
2405847
负责人:
LEO A PAQUETTE
金额:
$7.16万
依托单位:
依托单位国家:
美国
项目类别:
财政年份:
1995
资助国家:
美国
项目状态:
已结题
起止时间:
1995-01-15 至 1998-05-31
中文摘要
点击翻译按钮获取中文摘要
英文摘要
DESCRIPTION: Taxol and its close structural relatives represent very
demanding targets for the implementation of de novo synthetic tactics. This
is a consequence of their high structural complexity and abundant
stereochemical detail. The routes developed to the present time were
designed primarily to demonstrate that taxol can be prepared in the
laboratory. None can be categorized as particularly efficient. Seemingly
the best way to improve overall synthetic efficiency is to reduce the number
of requisite steps and utilize highly efficient processes. The primary goal
of the present effort is to develop an abbreviated route to taxol by
addressing at least two central rearrangements, which have been demonstrated
highly functionalized settings to be capable of meeting the stated needs.
The approach is therefore one designed around the tactic of elaborating the
entire taxane ring system early by submitting simple 1,2-adducts of
D-camphor derivatives to sequential charge-accelerated oxy-Cope and
alpha-ketol rearrangements alongside new, specifically tailored reactions.
A synthesis of taxusin, which takes advantage of many of these concepts, has
been completed.
The protocol will rely heavily on the use of D-camphor, an inexpensive,
enantiomerically pure commodity isolated from the camphor tree, in order to
produce the targeted compounds in their proper absolute configuration.
Emphasis is to be placed on brevity; consequently, very reasonable
regiocontrol and a minimum of protection/deprotection maneuvers are to be
deployed. Flexibility will also be paramount, such that minor changes in
methodology will allow for adaptation of the intermediates to arrival at
several targeted end-products.
The first priority is to arrive at taxol. Once the route to taxol is made
evident and is progressing well, real time will be devoted to structural
modifications. The ancillary objectives will include the preparation of
1-deoxytaxol and its alpha-oxetanyl isomer where the D ring is fused to the
alpha-surface of the framework.
期刊论文(0)
专著(0)
科研奖励(0)
会议论文
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:6416187
-
项目类别:
-
资助金额:$5.37万
-
财政年份:2000
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:6559330
-
项目类别:
-
资助金额:$6.2万
-
财政年份:2000
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:6027868
-
项目类别:
-
资助金额:$26.06万
-
财政年份:2000
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:6350406
-
项目类别:
-
资助金额:$25.97万
-
财政年份:2000
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:6628425
-
项目类别:
-
资助金额:$27.64万
-
财政年份:2000
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:6551975
-
项目类别:
-
资助金额:$1.75万
-
财政年份:2000
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:6497941
-
项目类别:
-
资助金额:$26.8万
-
财政年份:2000
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:2105131
-
项目类别:
-
资助金额:$24.13万
-
财政年份:1995
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:2008491
-
项目类别:
-
资助金额:$25.17万
-
财政年份:1995
-
负责人:LEO A PAQUETTE
-
依托单位:
TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
-
批准号:2105130
-
项目类别:
-
资助金额:$24.18万
-
财政年份:1995
-
负责人:LEO A PAQUETTE
-
依托单位:
MEDICINAL CHEMISTRY A STUDY SECTION
-
批准号:3555185
-
项目类别:
-
资助金额:$6.74万
-
财政年份:1986
-
负责人:LEO A PAQUETTE
-
依托单位:
SINGLE CRYSTAL X-RAY DIFFRACTION FACILITY
-
批准号:3519362
-
项目类别:
-
资助金额:$23.4万
-
财政年份:1986
-
负责人:LEO A PAQUETTE
-
依托单位:
MEDICINAL CHEMISTRY A STUDY SECTION
-
批准号:3555183
-
项目类别:
-
资助金额:$9.0万
-
财政年份:1986
-
负责人:LEO A PAQUETTE
-
依托单位:
SYNTHESIS OF UNUSUAL BIOLOGICALLY ACTIVE TERPENES
-
批准号:2175927
-
项目类别:
-
资助金额:$22.17万
-
财政年份:1983
-
负责人:LEO A PAQUETTE
-
依托单位:
SYNTHESIS OF UNUSUAL BIOLOGICALLY ACTIVE TERPENES
-
批准号:3278724
-
项目类别:
-
资助金额:$20.65万
-
财政年份:1983
-
负责人:LEO A PAQUETTE
-
依托单位:
SYNTHESES OF UNUSUAL BIOLOGICALLY ACTIVE TERPENES
-
批准号:3278722
-
项目类别:
-
资助金额:$16.66万
-
财政年份:1983
-
负责人:LEO A PAQUETTE
-
依托单位:
SYNTHESES OF UNUSUAL BIOLOGICALLY ACTIVE TERPENES
-
批准号:3278721
-
项目类别:
-
资助金额:$16.0万
-
财政年份:1983
-
负责人:LEO A PAQUETTE
-
依托单位:
SYNTHESIS OF UNUSUAL BIOLOGICALLY ACTIVE TERPENES
-
批准号:3278719
-
项目类别:
-
资助金额:$15.83万
-
财政年份:1983
-
负责人:LEO A PAQUETTE
-
依托单位:
SYNTHESES OF UNUSUAL BIOLOGICALLY ACTIVE TERPENES
-
批准号:3278723
-
项目类别:
-
资助金额:$17.7万
-
财政年份:1983
-
负责人:LEO A PAQUETTE
-
依托单位:
SYNTHESIS OF UNUSUAL BIOLOGICALLY ACTIVE TERPENES
-
批准号:3278725
-
项目类别:
-
资助金额:$21.44万
-
财政年份:1983
-
负责人:LEO A PAQUETTE
-
依托单位:
海外基金