61196-37-0Relevant articles and documents
CONJUGATES
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Page/Page column 77, (2020/07/14)
The present invention provides a conjugate of formula (I) and itsuse in methods of treatment, and also methods for delivering an active agent into a cell. The methods may be used to deliver an active agent into a nematode, flatworm, parasite or bacterium. The conjugate of formula (I) is: (formula (I)), wherein -D- is C1-4 alkylene or C2-4 alkenylene, preferably C2-4 alkenylene, where the alkylene or alkenylene is optionally substituted with alkyl or halo; A- is an active agent for delivery; and -RA, -RB, -RT1, -RT2, -R1, -R2, -R3, -X- and -L- are as defined herein.
Recovery preparation method of racepiquamine
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Paragraph 0080; 0081; 0082; 0085; 0087; 0089; 0091; 0093, (2018/06/12)
The invention discloses a recovery preparation method of racepiquamine-1. The preparation method comprises the following steps: dissolving a waste material S-piquamine intermediate-1 as an initial rawmaterial in a solvent; and carrying out reaction at a proper temperature in the presence of a catalyst and hydrogen at a certain pressure to prepare the piquamine intermediate-1 of racemate. The formula is as shown in the description. The configured piquamine S-1 which is not needed is efficiently, conveniently and fully operated and recovered with a high yield to obtain a racemate compound 1, and then the racemate compound is used again to prepare levopraziquantel, so that wastes can be turned into wealth, and therefore, the generation cost of the levopraziquantel is saved greatly.
Racemic praziquanamine recovery and preparation method
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Paragraph 0114; 0115; 0116; 0117; 0118; 0119; 0120-0141, (2017/09/19)
The present invention discloses a racemic praziquanamine-1 recovery and preparation method, which comprises: 1) preparing a compound 2 by using a waste material S-praziquanamine intermediate-1 as a starting raw material under the action of a catalyst or a dehydrogenation reagent; and 2) carrying out hydrogenation reduction on the compound 2 to obtain the racemic praziquanamine-1, wherein the formulas S-1, 1 and 2 are defined in the specification, the operations of the step 1) specifically comprise dissolving S-praziquanamine-1 in a first solvent, adding a first catalyst or a dehydrogenation reagent, and carrying out a reaction at a proper temperature to obtain the compound 2, and the operations of the step 2) specifically comprise dissolving the compound 2 in a second solvent, adding a second catalyst or a dehydrogenation reagent, and carrying out a reaction at a proper temperature to obtain the racemic praziquanamine-1. According to the present invention, the unwanted configuration praziquanamine S-1 is completely recovered and utilized to obtain the racemic compound 1, and the L-praziquantel is prepared by using the racemic compound 1 through the resolution method, such that the waste can be turned into treasure, and the L-praziquantel production cost can be substantially saved.