Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a -elimination mechanism.

Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a -elimination mechanism.

Disclosed herein, inter alia, are a process for the preparation of 2-bromolysergic acid diethylamide (2-Br-LSD), or a pharmaceutically acceptable salt thereof, via the controlled bromination of lysergic acid to form 2-bromolysergic acid, followed by amidation to form 2-Br-LSD, the purified 2-Br-LSD, per se, and pharmaceutical compositions containing the purified 2-Br-LSD, per se, and uses thereof.

Disclosed herein, inter alia, are a process for the preparation of 2-bromolysergic acid diethylamide (2-Br-LSD), or a pharmaceutically acceptable salt thereof, via the controlled bromination of lysergic acid to form 2-bromolysergic acid, followed by amidation to form 2-Br-LSD, the purified 2-Br-LSD, per se, and pharmaceutical compositions containing the purified 2-Br-LSD, per se, and uses thereof.

Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a -elimination mechanism.

Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a -elimination mechanism.

Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a -elimination mechanism.

Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a -elimination mechanism.

A process of synthesizing 2-bromo-LSD or a salt or hydrate thereof comprising the steps of reacting methylergometrine with a brominating agent to produce [(1S)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde as a first intermediate, and then hydrolyzing [(1S)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde to yield bromo-lysergic acid as a second intermediate, wherein bromo-lysergic acid is then amidated to yield 2-bromo-LSD or a salt or hydrate thereof.