Pyrrolopyrimidine Salt Crystal Forms for Solubility and Stability
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Solution Overview
Problem
Pyrrolopyrimidine compounds exhibit low solubility, which affects their chemical and physical stability, and there is a lack of reported salt or crystal forms that could improve these properties.
Innovation Solution
The development of salts and crystalline forms of pyrrolopyrimidine compounds, specifically with maleic acid, hydrochloric acid, and sulfuric acid, which enhance solubility, stability, and hygroscopicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If pyrrolopyrimidine compounds are used in their basic form, then they exhibit the desired biological activity, but they have low solubility which affects chemical and physical stability
Solution Approach 1:
The patent applies parameter changes by forming salts of pyrrolopyrimidine compounds with different acids (maleic acid, hydrochloric acid, sulfuric acid) to alter the chemical and physical properties of the compound. This salt formation changes the solubility parameters while maintaining the core biological activity, directly resolving the contradiction between stability and solubility
Solution Approach 2:
The patent creates composite material systems by combining pyrrolopyrimidine compounds with counterions from various acids to form salt compounds. These composite structures integrate the active pharmaceutical ingredient with stabilizing and solubility-enhancing components, simultaneously improving both stability and solubility characteristics
2Reliability
If pyrrolopyrimidine compounds are used in their basic form, then they maintain structural simplicity, but they lack the enhanced solubility and stability provided by salt or crystal forms
Solution Approach 1:
The patent modifies molecular parameters by forming salts without changing the core pyrrolopyrimidine structure. The salt formation adds counterions that improve stability while keeping the增加的 structural complexity minimal and localized to the ionic interactions rather than the core molecular framework
Data Source
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AI summary
Disclosed are a salt of a pyrrolopyrimidine compound, a crystalline form thereof, and an application thereof. Specifically provided are a crystal form of the compound represented by the formula I, a salt thereof, and a hydrate of the salt thereof, and a crystalline form of the compound represented by the formula (I), a method for preparation of the salt, and an application thereof; furthermore, the salt and crystalline form of the present invention are stable in nature and have good hygroscopicity, and have good prospects for finished-drug applications.