公开(公告)号：WO2014195896A1

公开(公告)日：2014-12-11

申请号：PCT/IB2014/061980

申请日：2014-06-05

Applicant: ANTHEM BIOSCIENCES PVT. LTD.

Inventor： GAVARA GOVINDA, Rajulu ,  SAMBASIVAM, Ganesh ,  PUTHIAPARAMPIL, Tom Thomas ,  CHANDRAPPA KORAMANGALA, Ravindra

IPC: C07C205/12 ,  C07C205/56 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07C201/08 ,  C07C205/56 ,  C07C205/12

Abstract: The present disclosure relates to compounds of Formula (I) and process of obtaining the same. Said compounds of Formula (I) is employed in the syntheses of pyrroloquinoline quinone (PQQ), 4,5-dioxo-4,5-dihydro-1H-pyrrolo[2,3-f]quinoline-2,7,9-tricarboxylic acid 2-allyl ester, 5-ethoxy-5-hydroxy-4-oxo-4,5-dihydro-1H-pyrrolo[2,3-f]quinoline-2,7,9-tricarboxylic acid, 5- hydroxy-6-(1,1,4-trioxo-1 lambda* 6*-1,2, 5 -thiadiazolidin-2-yl)-1H-indole-2-carboxylic acid and its pharmaceutically acceptable salts. Said syntheses of compounds via. compounds of Formula (I) as intermediates employ minimum number of steps resulting in a shorter process and has improved efficiency along with many other advantages.

Abstract translation: 本公开涉及式（I）的化合物及其获得方法。 所述式（I）化合物用于合成吡咯并喹啉醌（PQQ），4,5-二氧代-4,5-二氢-1H-吡咯并[2,3-f]喹啉-2,7,9-三羧酸 酸2-烯丙酯，5-乙氧基-5-羟基-4-氧代-4,5-二氢-1H-吡咯并[2,3-f]喹啉-2,7,9-三羧酸，5-羟基-6 - （1,1,4-三氧杂-1λ* 6 * -1,2,5-噻二唑烷-2-基）-1H-吲哚-2-羧酸及其药学上可接受的盐。 所述合成化合物通过。 作为中间体的式（I）化合物使用最少数量的步骤，导致更短的工艺并且具有改善的效率以及许多其它优点。

公开(公告)号：EP3004047B1

公开(公告)日：2017-02-22

申请号：EP14733718.2

申请日：2014-06-05

Applicant: Anthem Biosciences Pvt Ltd

Inventor： GAVARA GOVINDA, Rajulu ,  SAMBASIVAM, Ganesh ,  PUTHIAPARAMPIL, Tom Thomas ,  CHANDRAPPA KORAMANGALA, Ravindra

IPC: C07C201/08 ,  C07C205/56 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07C201/08 ,  C07C205/56 ,  C07C205/12

公开(公告)号：EP3004047A1

公开(公告)日：2016-04-13

申请号：EP14733718.2

申请日：2014-06-05

Applicant: Anthem Biosciences Pvt Ltd

Inventor： GAVARA GOVINDA, Rajulu ,  SAMBASIVAM, Ganesh ,  PUTHIAPARAMPIL, Tom Thomas ,  CHANDRAPPA KORAMANGALA, Ravindra

IPC: C07C205/12 ,  C07C205/56 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07C201/08 ,  C07C205/56 ,  C07C205/12

Abstract: The present disclosure relates to compounds of Formula (I) and process of obtaining the same. Said compounds of Formula (I) is employed in the syntheses of pyrroloquinoline quinone (PQQ), 4,5-dioxo-4,5-dihydro-1H-pyrrolo[2,3-f]quinoline-2,7,9-tricarboxylic acid 2-allyl ester, 5-ethoxy-5-hydroxy-4-oxo-4,5-dihydro-1H-pyrrolo[2,3-f]quinoline-2,7,9-tricarboxylic acid, 5- hydroxy-6-(1,1,4-trioxo-1 lambda* 6*-1,2, 5 -thiadiazolidin-2-yl)-1H-indole-2-carboxylic acid and its pharmaceutically acceptable salts. Said syntheses of compounds via. compounds of Formula (I) as intermediates employ minimum number of steps resulting in a shorter process and has improved efficiency along with many other advantages.

Abstract translation: 新化合物3（3-（5- substituiertem氧基-2,4-二硝基 - 苯基）-2-氧代 - 丙酸酯）的合成使吡咯喹啉醌（PQQ），并使用它用于制药目的进行说明。 更具体地，本公开涉及通过使用新的中间体：式1在较短的处理和PQQ的更高的产率得到的在有效的方法在合成PQQ。 独特的工艺，使用要么氢氧化钠和/或碳酸钠的PQQ化合物钠因此被示出。