PRODRUGS AND DRUG-MACROMOLECULE CONJUGATES HAVING CONTROLLED DRUG RELEASE RATES
申请人:PROLYNX LLC
公开号:US20140296476A1
公开(公告)日:2014-10-02
The present invention provides methods and compositions that permit controlled and prolonged drug release in vivo. The compounds are either prodrugs with tunable rates of release, or conjugates of the drug with macromolecules which exhibit tunable controlled rates of release.
Selective mono- and dialkenylation of N-acetylcarbazoles was achieved by using Cp*Rh(III)- and CpERh(III)-catalysts, respectively. Unexpectedly, the dialkenylation was accompanied by the removal of acetyl directing group to produce 1,8-dialkenyl-N-H-carbazoles.
N-乙酰咔唑的选择性单烯基化和二烯基化分别通过使用 Cp*Rh(III)- 和 Cp E Rh(III)- 催化剂实现。出乎意料的是,二烯基化伴随着乙酰基导向基团的去除,产生 1,8-二烯基-N -H-咔唑。
Mazzara; Leonardi, Gazzetta Chimica Italiana, 1895, vol. 25 II, p. 397