- A Three-Step Synthesis of δ-Aminolaevulinic Acid
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Piperidine-2,5-dione (4) is prepared by catalytic hydrogenation of 5-hydroxy-2-pyridone (3).Ring opening of the lactam 4 with concentrated hydrochloric acid yields the hydrochloride of δ-aminolaevulinic acid (2).
- Herdeis, Claus,Dimmerling, Anna
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- CRYSTAL FORM I OF A 5-AMINOPYRAZOLE CARBOXAMIDE COMPOUND AS BTK INHIBITOR
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Disclosed is a new crystal form of a 5-aminopyrazole carboxamide compound as shown in Formula (I). Also disclosed are a preparation method for said crystal form of said compound, a pharmaceutical composition of said crystal form of said compound, and uses thereof.
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Paragraph 0036; 0041
(2020/09/23)
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- N-SUBSTITUTED TETRAHYDROTHIENOPYRIDINE DERIVATIVES AND USES THEREOF
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A compound of Formula (I) is provided that has been shown to be useful for treating a disease caused by a viral infection: (I) wherein R1, R2, R3, A, L, m, n, p and q are as defined herein.
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- 5-AMINOPYRAZOLE CARBOXAMIDE DERIVATIVE AS BTK INHIBITOR AND PREPARATION METHOD AND PHARMACEUTICAL COMPOSITION THEREOF
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The present application discloses novel 5-aminopyrazole carboxamide compounds as shown in formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof. In addition, the present application further discloses a method for the preparation of the compounds, a pharmaceutical composition comprising a compound of the invention and the use of the compounds.
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Paragraph 0084
(2019/04/16)
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- Preparation method of 2,5-piperidione
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The invention relates to a preparation method of 2,5-piperidione. 2-glutamic acid is used as a starting raw material to perform closed loop reaction to produce a compound 2 under the effects of NaNO2; a compound 3 is produced through borane reduction; a compound 4 is produced under the effects of methylsufonyl chloride; a compound 5 is produced through substitution under the sodium azide effect; a compound 6 is produced through Pd/H2 under the reduction effect; a target compound is generated under the effect of Dess-Martin periodinane. The preparation method has the advantages that the raw materials are cheap and can be easily obtained; the synthetic method is simple; the method belongs to a fire-new method for synthesizing 2,5-piperidione. The method meets the requirements of large-scale industrial production.
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- TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS
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Compounds of Formula (I) are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula (I) have the above structure, where the definitions of the variables are provided herein.
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Page/Page column 205-206
(2013/02/28)
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- Deoligomerization: a new route to lactams from unsaturated amides via radical oligomerization.
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[reaction: see text] Triethylborane-initiated atom transfer radical oligomerization of N-allyl or N-(3-butenyl)iodoacetamides followed by treatment with hydrochloric acid and subsequent neutralization with K(2)CO(3) led to the formation of the corresponding 5-hydroxyl-substituted delta-lactams or caprolactams, respectively. This oligomerization-deoligomerization sequence serves as an alternative to the corresponding intramolecular cyclization reactions.
- Liu,Wang, Xing,Li, Chaozhong
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p. 361 - 363
(2007/10/03)
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