1. Lowering LogD to increase water solubility Changing the carbonyl group and kai-dimethyl in the molecule to oxetane can reduce LogD and increase water solubility . Introducing oxetane at different positions in the molecule has different effects on LogD and water solubility. 2. Effect on pKa The polar nature of oxetane can be used to modulate the base of the proximal amine. pKa decreases depending on the topological distance between the two functional units. When the methylene unit is replaced by an oxetane unit, the amino group at the α-position shows the largest decrease in pKa (between -2.5 and -3.5). 3. Substitution of morpholine or other carbonyl-based structures in the block The aqueous solubility of lipophilic scaffolds is often improved by the incorporation of morpholine structures, even though it is known that morpholine may be a target for oxidative metabolism. There are 17 commercially available APIs that contain a morpholine fraction. Metabolic data have been published for 13 of these compounds, and oxidative degradation of the morpholine peptide ring is the major metabolic pathway in eight of them. Spiro epoxetanes can be regarded as structural analogues of morpholine because of their ability to increase solubility while maintaining stability in oxidative metabolism. Thus, these oxetane derivatives are known as useful alternative building blocks to morpholine or other carbonyl-like structures through their unique polar spatial distribution. 4. Substitution of morpholine or other carbonyl-based structures in the block The aqueous solubility of lipophilic scaffolds is often improved by the incorporation of morpholine structures, even though it is known that morpholine may be a target for oxidative metabolism. There are 17 commercially available APIs that contain a morpholine fraction. Metabolic data have been published for 13 of these compounds, and oxidative degradation of the morpholine peptide ring is the major metabolic pathway in eight of them. Spiro epoxetanes can be regarded as structural analogues of morpholine because of their ability to increase solubility while maintaining stability in oxidative metabolism. Thus, these oxetane derivatives are known as useful alternative building blocks to morpholine or other carbonyl-like structures through their unique polar spatial distribution.

지금 문의하세요!

가격이 필요한 경우 아래 양식에 연락처 정보를 입력해 주시면 보통 24시간 이내에 연락드리겠습니다. 이메일을 보내셔도 됩니다. info@changhongchemical.com 근무 시간(오전 8시 30분~오후 6시, 월~토요일)에 문의하거나 웹사이트 라이브 채팅을 이용하면 신속하게 답변을 받을 수 있습니다.

Related product references: For formulation review or sourcing comparison, see CHLUMICRYL 201 및 CHLUMICRYL 203.