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Cyclic α-n-Protected Amino Ester Formation of n-Protected Bis-3,6-(4-aminobutyl)-2,5-piperazinedione

A technology of aminoalkyl and active amino esters, applied in the field of bioactive agents, improved synthesis, and delivery of active agents, which can solve the problems of difficult manufacture, poor stability, and unavailability of the system

Active Publication Date: 2021-06-15
MANNKIND CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, broad-spectrum use of drug delivery systems has been prevented for a number of reasons including: (1) the system requires toxic amounts of adjuvants or inhibitors; (2) suitable low molecular weight carriers (i.e., active agents) are not available; ( 3) the system exhibits poor stability and insufficient shelf life; (4) the system is difficult to manufacture; (5) the system cannot protect the active agent (carrier); (6) the system negatively alters the active agent; or (7) the system cannot Allow or facilitate absorption of active agents

Method used

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  • Cyclic α-n-Protected Amino Ester Formation of n-Protected Bis-3,6-(4-aminobutyl)-2,5-piperazinedione
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  • Cyclic α-n-Protected Amino Ester Formation of n-Protected Bis-3,6-(4-aminobutyl)-2,5-piperazinedione

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Experimental program
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Embodiment

[0077]figure 1 A reactive amino ester for use by cyclic alpha-N-N-N-N-N figure 1 The CBZ-Lys-NCA shown is produced by the reaction flow of the compound 11. Synthesis of CBZ-Lys-NCA according to the following procedure: Tribe (26.49 g), CBZ-Lys (50.00 g) and tetrahydrofuran (THF) (500ml) were injected with nitrogen purge, mechanical agitator, condenser and thermocouple. 1L 4-neck round bottom flask. The reaction mixture was heated to 35-38 ° C until it was clarified. The reaction mixture was cooled to ambient temperature, and the nitrogen bubble was bubbled through the reaction mixture to remove any excess of inert gas. The solvent was then removed in vacuo. The crude product was crystallized from THF (200 mL) and hexane (125 mL). The isolated white solids were dried overnight overnight with filtration and in vacuo. The yield of CBZ-Lys-NCA was 48.6 g (89.02%).

[0078] Once CBZ-Lys-NCA is obtained, it is used to generate compound 11 below: injecting a benzylamine catalyst (3.33 g)...

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Abstract

Methods are provided for the synthesis of N-protected 3,6-aminoalkyl-2,5-piperazinediones. The method comprises obtaining a cyclic α-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.

Description

[0001] This application is the application date, 2014, 2014, 201480015534.X, inventive name * # * Protected amino ester forming N-protected dual-3,6- (4-aminitrigopyrous "by a cyclic α-N-protected amino Basis) -2,5-Piperazine Diaclone * # * 'Patent Application. [0002] Related application cross-reference [0003] The present non-provisional patent application requires priority to the US Provisional Application Serial No. 61 / 798,016, which is incorporated herein by reference. It is intended to be in this article. Technical field [0004] The present invention relates to a composition for delivering an active agent, in particular a biologically active agent. The disclosed embodiments belong to the field of chemical synthesis, and more particularly to a modified synthesis method for preparing a substituted piperazine. Background technique [0005] Drug delivery is a continuation of the active agent to the patient. Conventional methods for delivering active agents are often severe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D241/08A61K47/22
CPCA61K47/22C07D241/08C07D241/10C07D241/04
Inventor J.J.弗里曼O.凡斯蒂尔W.E.贝K.S.克拉夫特
Owner MANNKIND CORP