- Preparation method of chiral morpholine compound
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The invention provides a preparation method of a chiral morpholine compound. With chiral ethylene oxide as a raw material, the preparation method comprises the steps of ring opening, cyclization and deprotection reaction to obtain the chiral 2-substituted morpholine compound. The preparation process is simple and environmentally friendly, has mild reaction conditions, is free of irritation or allergens, has higher total yield and good safety and is suitable for industrial amplification.
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Paragraph 0086; 0088; 0093
(2018/10/11)
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- A concise and efficient synthesis of substituted morpholines
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A simple and efficient method has been developed for the synthesis of substituted morpholines by a sequence of coupling, cyclization, and reduction reactions of easily available amino alcohols and α-halo acid chlorides. Various mono-, di-, and trisubstituted morpholines, spiro morpholines, and ring-fused morpholines, as well as morpholine homologues, were synthesized in good to excellent yields by a single methodology under similar reaction conditions. The method was also used in a multigram synthesis of (3S)-3-methylmorpholine.
- Dugar, Sundeep,Sharma, Amit,Kuila, Bilash,Mahajan, Dinesh,Dwivedi, Sandeep,Tripathi, Vinayak
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- DIBENZOTHIOPHENE DERIVATIVES AS DNA- PK INHIBITORS
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Compound formula I: wherein: X1 and X2 may be either (a) C and O, (b) N and N, or (c) C and NH, where the dotted bonds represents a double bond in the appropriate location; R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, or an optionally substituted C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; RN1 is selected from hydrogen and an optionally substituted C1-4 alkyl group; RC1 is selected from an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, or an optionally substituted C5-20 aryl group; or RN1 and RC1 may together form an optionally substituted C2-4 alkylene group.
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Page/Page column 86
(2010/12/26)
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- Diastereoselective synthesis of enantiopure morphelines by electrophilic selenium-induced 6-exo cyclizations on chiral 3-allyl-2-hydroxymethylperhydro-1, 3-benzoxazine derivatives
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Enantiopure morpholine derivatives have been prepared by selenocyclofunctionalization of chiral 3-allyl-2-hydroxymethyl-substituted perhydro-1,3-benzoxazine derivatives. The cyclization occurs in high yields and diastereoselection, although the temperature of the reaction and the structure of the substituent at C-2 and the substitution pattern of the double bond can modify the regio- and stereochemistry of the final products.
- Pedrosa, Rafael,Andres, Celia,Mendiguchia, Pilar,Nieto, Javier
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p. 8854 - 8863
(2007/10/03)
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