147081-49-0Relevant articles and documents
Preparation method of ceftobiprole ester intermediate (R)-1-tert-butyloxycarbonyl-3-aminopyrrolidine
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Paragraph 0035; 0050-0057; 0073-0078-0079; 0095-0100, (2020/09/08)
The invention discloses a preparation method of (R)-1-tert-butyloxycarbonyl-3-aminopyrrolidine. The method comprises the following steps: 1, carrying out a reaction on (D) asparagine with thionyl chloride/methanol to generate D-asparagine methyl ester hydrochloride; protecting the amino group of the D-aspartic acid methyl ester hydrochloride by using di-tert-butyl dicarbonate; carrying out a ringclosing reaction by using sodium hydride, removing BOC anhydride protection of 3-amino by using TFA, and then reducing the diketone at the 2 and 5 sites by using sodium borohydride; finally protecting1-imino by using di-tert-butyl dicarbonate to obtain an yellow oily substance, (R)-1-tert-butyloxycarbonyl-3-aminopyrrolidine. The method is low in cost, small in pollution, easy to operate and beneficial to industrial production, the purity of the product can reach 98%, and a guarantee is provided for subsequent synthesis of high-purity cefepime.
Aromatic heterocyclic derivatives and applications of aromatic heterocyclic derivatives in medicines
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, (2016/10/09)
The present invention discloses aromatic heterocyclic derivatives and applications of the aromatic heterocyclic derivatives in medicines, and specifically provides a class of aromatic heterocyclic compounds or stereoisomers, geometric isomers, tautomers, racemic bodies, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the compounds. The present invention further discloses uses of the compounds or pharmaceutical compositions in drug preparation, wherein the drug is used for treatment of respiratory diseases, particularly chronic obstructive pulmonary disease (COPD).
NOVEL 7-SUBSTITUTED 3-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS
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Page/Page column 50, (2009/09/08)
A subject of the invention is the compounds of formula (I): in which either R1 represents H, OH, NH2, —(CH2)m—NRaRb(m=0.1 or 2),Ra and Rb represent H, linear, branched or cyclic (C1 -C6) alkyl, (C3-C6) cycloalkyl-(C3-C6)— alkyl, Rc, S(O)2Rc, C(O)Rc, S(O)2Rd or C(O)Rd;or Ra and Rb with N form an Rc radical;Rc represents a saturated, unsaturated or 5- or 6-members aromatic ring, containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted;Rd represents a linear, branched or cyclic (C1-C6) alkyl, optionally substituted by 1 to 4 halogens;or R1 represents Rc or CHReRc or CHReRd;Re represents H, OH, NH2, NH—(C1-C6)-alk or N-(C1-C6)-alk2, or NH—(C1-C7)-acyl or NHRc;R2 represents H, (CH2)m—NRaRb, Rc, CHReRc or CHReRd, and R′2 represents H; it being understood that R1 and R2 cannot at the same time be H or that R1 and R2 or R2 and R1 cannot be one (CH2)m—NRaRb or Rc or H and the other one OH, or one H and the other one NH2, or one H and the other one (CH2)m—NRaRb in which Ra and Rb represent H or alkyl or C(O)Rd, in which Rd represents an unsubstituted alkyl or cycloalkyl; or R1 has the above definition except H and R2 and R′2 together represent gem dialkyl or alkyl-oxime, or R2 and R′2 represent respectively Rc or Rd and OH, NH2, NHRc or NHRf, Rf being a (C1-C7) acyl radical;or R1 represents H and R2 and R′2 together represent alkyl-oxime or one represents Rc and the other one represents OH, NH2, NHRc or NHRf;n is 0 or 1;R3 and R′3 represent H or (C1-C6) alkyl optionally substituted by 1 to 3 halogens or R3 represents (C1-C6) alkoxy carbonyl and R′3 represents H;R4 represents methyl optionally substituted by halogen;R5 represents H, (C1-C6) alkyl or (C7-C12) arylalkyl;R6 represents H, fluorine, NO2, CF3 or CN;in the form of enantiomers or mixtures, as well as their salts with acids and bases; their preparation and their application as anti-bacterials, in both human and veterinary medicine.
