A Pd-catalyzed reaction of vinyl iodides and N-tosylhydrazones that assembles eta(3)-allyl ligands through carbene insertion is demonstrated. Intramolecular trapping with nitrogen nucleophiles generates good yields of cinnamyl and pentadienyl amines like those found in alkaloid natural products. Carbenylative amination was the key reaction to complete the synthesis of the alkaloid caulophyllumine B. Migratory insertion was biased to provide allylamines with optical purity up to 64% ee, but in a lower yield.
METHODS AND COMPOSITIONS FOR MAKING AN AMINO ACID TRIISOCYANATE
申请人:Warsaw Orthopedic, Inc.
公开号:US20150197488A1
公开(公告)日:2015-07-16
A method of making an amino acid triisocyanate is provided, the method comprising reacting an amino acid trihydrochloride with phosgene to form the amino acid triisocyanate. In some embodiments, the amino acid trihydrochloride comprises lysine ester trihydrochloride salt and the amino acid triisocyanate comprises lysine ester triisocyanate. In some embodiments, there is a lysine ester triisocyanate having a purity of at least about 98%, the lysine ester triisocyanate having a structure resulting from reacting lysine ester trihydrochloride salt with phosgene to form the lysine ester triisocyanate. These lysine ester triisocyanates can be used to make biodegradable polyurethanes.
METHODS AND COMPOSITIONS FOR MAKING AN AMINO ACID TRIHYDROCHLORIDE
申请人:Warsaw Orthopedic, Inc.
公开号:US20150197483A1
公开(公告)日:2015-07-16
In some embodiments, a method of making an amino acid trihydrochloride is provided, the method comprising reacting an amino acid monohydrochloride with an alkanolamine to form the amino acid trihydrochloride. In some embodiments, the amino acid monohydrochloride comprises lysine hydrochloride, which is mixed with ethanolamine to form lysine ester trihydrochloride. In some embodiments, there is a lysine ester trihydrochloride salt having a purity of at least about 98%, the lysine ester trihydrochloride salt having a structure resulting from reacting lysine hydrochloride and ethanolamine to form the lysine ester trihydrochloride salt. The lysine ester trihydrochloride can be made in one reaction vessel.
The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same. Compositions herein are useful for drug-delivery applications.
HYBRID BLOCK COPOLYMER MICELLES WITH MIXED STEREOCHEMISTRY FOR ENCAPSULATION OF HYDROPHOBIC AGENTS
申请人:SILL Kevin N.
公开号:US20080274173A1
公开(公告)日:2008-11-06
The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same.
本发明涉及聚合物化学领域,更具体地说是涉及多嵌段共聚物以及包含该共聚物的胶束。
Therapy
申请人:——
公开号:US20030225111A1
公开(公告)日:2003-12-04
The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q
1
includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q
3
—X
1
— wherein X
1
includes a direct bond and O and Q
3
includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R
2
and R
3
is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q
2
includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human.
1