167298-58-0Relevant articles and documents
Synthesis of Guanine α-Carboxy Nucleoside Phosphonate (G-α-CNP), a Direct Inhibitor of Multiple Viral DNA Polymerases
Maguire, Nuala M.,Ford, Alan,Balzarini, Jan,Maguire, Anita R.
, p. 10510 - 10517 (2018)
The synthesis of guanine α-carboxy nucleoside phosphonate (G-α-CNP) is described. Two routes provide access to racemic G-α-CNP 9, one via base construction and the other utilizing Tsuji-Trost allylic substitution. The latter methodology was also applied to the enantiopure synthesis of both antipodes of G-α-CNP, each of which showing interesting antiviral DNA polymerase activity. Additionally, we report an improved multigram scale preparation of the cyclopentene building block 10, starting material for the preferred Tsuji-Trost route to 9.
Asymmetric Phase-Transfer Catalytic aza-Michael Addition to Cyclic Enone: Highly Enantioselective and Diastereoselective Synthesis of Cyclic 1,3-Aminoalcohols
Lee, Jaeyong,Ban, Jeong Woo,Kim, Jeongseok,Yang, Sehun,Lee, Geumwoo,Dhorma, Lama Prema,Kim, Mi-Hyun,Ha, Min Woo,Hong, Suckchang,Park, Hyeung-Geun
, p. 1647 - 1651 (2022/03/03)
The highly enantioselective aza-Michael reaction of tert-butyl β-naphthylmethoxycarbamate to cyclic enones has been accomplished by using a new cinchona alkaloid derived C(9)-urea ammonium catalyst under phase-transfer catalysis conditions with up to 98% ee at 0 °C. The resulting aza-Michael adducts can be converted to versatile intermediates by selective deprotection and the cyclic 1,3-aminoalcohols by diastereoselective reduction with up to 32:1, which have been widely used as important pharmacophores in pharmaceutical development.
KRAS G12C Inhibitor compound and application thereof
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Paragraph 0141-0142; 0146-0148, (2021/05/12)
The invention provides a KRAS G12C inhibitor compound and an application thereof, and particularly provides a compound as shown in a formula (I), and an optical isomer, a hydrate, a solvate or pharmaceutically acceptable salt thereof. The compound can be used as a KRAS G12C inhibitor and is used for treating diseases related to the activity or expression quantity of KRAS G12C.
Preparation method of (1R,3S)-3-aminocyclopentanol and intermediate thereof
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, (2020/05/05)
The invention discloses a preparation method of (1R,3S)-3-aminocyclopentanol and an intermediate thereof. The invention provides a preparation method of a compound as shown in a formula I'-1. The preparation method comprises a step: re-crystallizing a mixture of compounds as shown in the formula I'-1 and the formula I'-2 in a solvent, wherein the solvent is a mixed solvent of a poor solvent and agood solvent, the poor solvent is a ketone solvent and methanol, and the good solvent is water. The preparation method is high in reaction yield, and a single-configuration product with high optical purity can be obtained.
Preparation method of (1R,3S)-3-amino-1-cyclopentanol and salt thereof
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Paragraph 0163-0169, (2020/03/16)
The invention discloses a preparation method of (1R,3S)-3-amino-1-cyclopentanol and a salt thereof, and relates to the field of organic synthesis. In the method, a chiral source in an N-Acyl hydroxylamine compound is used as chiral induction, and an asymm
Preparation of optically-pure cyclic amino alcohol and salt thereof
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Paragraph 0093-0104, (2020/01/12)
The invention relates to the field of chemical pharmacy, in particular to a method for preparing an optically-pure cyclic amino alcohol and a salt thereof. The method comprises: 1) catalytic hydrogenation: a compound (12) is subjected to catalytic hydroge
Preparation method of optically pure cyclic amino alcohol and salt thereof
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Paragraph 0098-0103, (2020/01/25)
The invention relates to the field of chemical pharmacy, particularly to a preparation method of optically pure cyclic amino alcohol and a salt thereof. The method comprises 1) hydrolysis: hydrolyzinga compound (12) to obtain a compound (13), and 2) catalytic hydrogenation: carrying out catalytic hydrogenation on the compound (13) obtained in the hydrolysis step to obtain a compound (1).
Method for preparing single-configuration 3-aminocyclopentanol through chiral resolution
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, (2019/08/12)
The invention relates to a method for preparing a single-configuration 3- aminocyclopentanol through chiral resolution. Specifically, the invention discloses a chiral splitting method of 3-aminocyclopentanol. The preparation method is simple to operate, a
A (1 R, 3 S) -3 - amino-cyclopentanol hydrochloride preparation method (by machine translation)
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Paragraph 0034; 0038, (2019/05/08)
The invention discloses a (1 R, 3 S) - 3 - amino-cyclopentanol hydrochloride of the preparation method, the method using chiral carboxylic acid with hydroxylamine to form the amide as chiral source, in copper catalyzed oxidation in the reaction system to rapidly obtain a chiral Diels - alder reaction product, after passes through the reduction reaction and alkaline deprotection reaction, and acidified after reaction to obtain the target product. Chiral inducing reagent chiral carboxylic acid by simple acidification, extraction processing can be reclaimed and reused. This kind of (1 R, 3 S) - 3 - amino-cyclopentanol hydrochloride preparation method has high operation safety and high selectivity, raw materials are easy, and the cost is low, the reaction time is short and simple process flow and the like. (by machine translation)
Intermediate for preparing bictegravir and preparation method thereof
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Paragraph 0110; 0111, (2019/01/08)
The invention relates to the technical field of a drug, and concretely relates to an intermediate for preparing bictegravir and a preparation method thereof. The present invention provides two novel types of compounds and three routes for preparation of a compound (VI). Through substrate induction, chiral catalysis or synergistic effect of substrate induction and chiral catalysis, the stereoselectivity of a Diels-Alder reaction can be greatly improved, and a high chiral purity of a common intermediate (III) can be obtained; cut-out of N-O bond and reduction the double bond use catalytic hydrogenation, which can be environmentally friendly; the reaction conditions are mild, the yield is higher than the existing preparation method, the method is economic and effective, and is adapted to large-scale industrial production.