- Syntheses of morpholine-2,3-diones and 2-hydroxymorpholin-3-ones: Intermediates in the synthesis of aprepitant
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The preparation of morpholine-2,3-diones and 2-hydroxymorpholin-3-ones from N-substituted β-amino alcohols is reported. These were useful intermediates in the synthesis and development of aprepitant.
- Nelson, Todd D.,Rosen, Jonathan D.,Brands, Karel M.J.,Craig, Bridgette,Huffman, Mark A.,McNamara, James M.
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- Skin
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PROBLEM TO BE SOLVED: To provide a skin care preparation suitable for a cosmetic (provided that quasi drugs are included) or the like, for detail, a skin care preparation having whitening effects, particularly preventive or improving effects against pigme
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Paragraph 0058
(2018/03/23)
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- Skin care
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PROBLEM TO BE SOLVED: To provide a skin care preparation suitable for a cosmetic (provided that quasi drugs are included) or the like, for detail, a skin care preparation having whitening effects, particularly preventive or improving effects against pigme
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Page/Page column 0057; 0059
(2017/10/05)
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- Skin care
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PROBLEM TO BE SOLVED: To provide a skin care preparation suitable as a cosmetic (including quasi medicine), etc.SOLUTION: The skin care preparation comprises an acyl derivative of serine and a compound represented by the general formula [wherein Ris an un
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Paragraph 0115-0118
(2020/10/19)
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- Preparation of N-arylmethyl aziridine derivatives, 1,4,7,10-tetraazacyclododecane derivatives obtained therefrom and N-arylmethyl-ethanol-amine sulphonate esters as intermediates
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PCT No. PCT/GB96/00552 Sec. 371 Date Dec. 2, 1997 Sec. 102(e) Date Dec. 2, 1997 PCT Filed Mar. 8, 1996 PCT Pub. No. WO96/28420 PCT Pub. Date Sep. 19, 1996Aziridines may be subjected to a cyclooligomerization reaction to produce polyazacycloalkane compounds useful for example in the preparation of chelating agents for use in diagnostic imaging contrast agents. N-benzyl-aziridine in particular is useful as it can be cyclotetramerized and debenzylated to yield cyclen, a key intermediate in chelating agent preparation. The invention provides a particularly attractive route to production of N-benzyl and other N-arylmethyl aziridines of formula (I) where each R1 is independently hydrogen or a group AR and Ar is an optionally substituted phenyl group. The process comprises reacting a purified N-arylmethylethanolaminesulphonate ester with a base. N-arylmethyl-ethanolamine sulphonate ester of the formula R'NHCH2CH2OSO3H, wherein the N-arylmethyl group R' is an N-(bisarylmethyl) or N-(triarylmethyl) group, as intermediates. In a further aspect, the invention provides compounds of formula (II) where Ar and R1 are as hereinabove defined and at least two differing ArCHR21 moieties are present.
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