- New route for the synthesis of chiral hydrazine SADP
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A convenient route for the synthesis of (S)-1-amino-2-(1-methoxy-1- methylethyl)pyrrolidine (SADP) was established. The route involved three key steps viz. the Grignard addition to the N-Boc-proline ester (1), nitrosation to the aminoalcohol hydrochloride (3) and O-methylation to the alcohol group of N-nitrosopyrrolidine (4). (S)-1,1-dimethyl-tetrahydropyrrolo[1,2-c]oxazol-3-one (6) was also obtained via the reaction of (S)-1-Boc-2-(1-hydroxy-1-methylethyl) pyrrolidine (2) with sodium hydride.
- Jia, Tao
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- Chiral binaphthalene-aza-polycyclic ligand and preparation method thereof
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The invention discloses a chiral binaphthalene aza-polycyclic ligand and a preparation method thereof. The ligand has the following structure. The preparation method comprises the following steps: (1)by taking 1, 1 '-binaphthalene 2, 2'-diphenol as a raw material, carrying out methyl protection, Tf2O protection, methylation, aromatic ring substitution and bromination reaction to obtain a 2-bromomethyl -2'-methoxy 1, 1'-binaphthalene derivative (compound V); (2) starting from aza-polycyclic carboxylic acids such as L -or D-proline, L -or D-2-piperidinecarboxylic acid, L- or D-acridine -acid and the like, carrying out derivatization to obtain various amino alcohols (compounds B); and (3) coupling the compound V and the compound B under an alkaline condition and a catalyst, and removing a protecting group to obtain the binaphthalene aza-polycyclic chiral ligand L. The ligand has central chirality and axial chirality at the same time, and can obtain higher reaction activity and enantioselectivity in asymmetric catalytic reaction. The ligands are simple to prepare, raw materials are easy to obtain, and the ligands have important significance for asymmetric synthesis.
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- Novel chiral amine oxide ligand and preparation method thereof
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The invention provides a novel chiral amine oxide ligand and a preparation method thereof. The method uses a simple amino acid or an amino acid derivative as a raw material, the raw material is modified, the modified material reacts with substances such as a coupling agent and an alkali, and therefore the pincher configuration chiral ligand compound is obtained, that is, the chiral amine oxide ligand. The chiral amine oxide ligand provided by the invention has a structure of a non-simple linear chain, has a soft skeleton in the molecular structure, contains a recognition gene containing heteroatoms such as oxygen or nitrogen, and can well coordinate with a series of metals and realize high enantioselectivity and high reactivity in a non-symmetric reaction; and the preparation method is simple, the steps are few, and the raw materials are cheap and easy to obtain.
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- C-3 NOVEL TRITERPENONE WITH C-28 AMIDE DERIVATIVES AS HIV INHIBITORS
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The invention relates to C-3 novel triterpenone with C-28 amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases (formula 1).
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Paragraph 0150
(2018/09/12)
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- NOVEL BETULINIC SUBSTITUTED AMIDE DERIVATIVES AS HIV INHIBITORS
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The present invention relates to novel betulinic substituted amide compounds of formula (I); and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y, Z1, Z2, Z3 and are Formula (II) as defined herein. The invention novel betulinic substituted amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
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Page/Page column 61-62
(2017/02/24)
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